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Pk11195

CAS No.:
85532-75-8
Catalog Number:
AG004R3B
Molecular Formula:
C21H21ClN2O
Molecular Weight:
352.8572
Pack Size
Purity
Availability
Location
Price(USD)
Quantity
  
5mg
99%
1 week
United States
$133
- +
10mg
≥98%
1 week
United States
$139
- +
50mg
≥98%
1 week
United States
$344
- +
100mg
99%
1 week
United States
$682
- +
Product Description
Catalog Number:
AG004R3B
Chemical Name:
Pk11195
CAS Number:
85532-75-8
Molecular Formula:
C21H21ClN2O
Molecular Weight:
352.8572
MDL Number:
MFCD00069334
IUPAC Name:
N-butan-2-yl-1-(2-chlorophenyl)-N-methylisoquinoline-3-carboxamide
InChI:
InChI=1S/C21H21ClN2O/c1-4-14(2)24(3)21(25)19-13-15-9-5-6-10-16(15)20(23-19)17-11-7-8-12-18(17)22/h5-14H,4H2,1-3H3
InChI Key:
RAVIZVQZGXBOQO-UHFFFAOYSA-N
SMILES:
CCC(N(C(=O)c1cc2ccccc2c(n1)c1ccccc1Cl)C)C
Properties
Complexity:
457  
Compound Is Canonicalized:
Yes
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
0
Defined Bond Stereocenter Count:
0
Exact Mass:
352.134g/mol
Formal Charge:
0
Heavy Atom Count:
25  
Hydrogen Bond Acceptor Count:
2  
Hydrogen Bond Donor Count:
0
Isotope Atom Count:
0
Molecular Weight:
352.862g/mol
Monoisotopic Mass:
352.134g/mol
Rotatable Bond Count:
4  
Topological Polar Surface Area:
33.2A^2
Undefined Atom Stereocenter Count:
1  
Undefined Bond Stereocenter Count:
0
XLogP3:
5.5  
Literature
Title Journal
Human pregnane X receptor is activated by dibenzazepine carbamate-based inhibitors of constitutive androstane receptor. Archives of toxicology 20170601
Propagation of damage in the rat brain following sarin exposure: Differential progression of early processes. Toxicology and applied pharmacology 20161101
Improved assays for xenosensor activation based on reverse transfection. Toxicology in vitro : an international journal published in association with BIBRA 20151001
Chrysin, baicalein and galangin are indirect activators of the human constitutive androstane receptor (CAR). Toxicology letters 20150304
Proteasomal interaction as a critical activity modulator of the human constitutive androstane receptor. The Biochemical journal 20140215
Release of targeted p53 from the mitochondrion as an early signal during mitochondrial dysfunction. Cellular signalling 20131201
Identification of potent Yes1 kinase inhibitors using a library screening approach. Bioorganic & medicinal chemistry letters 20130801
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds. European journal of medicinal chemistry 20130501
Imaging microglial activation and glucose consumption in a mouse model of Alzheimer's disease. Neurobiology of aging 20130101
TO901317, a potent LXR agonist, is an inverse agonist of CAR. The Journal of toxicological sciences 20130101
A translocator protein ligand PK11195 shows antigrowth activity in human choriocarcinoma cells. Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine 20121001
Design, synthesis and structure-activity relationships of novel benzoxazolone derivatives as 18 kDa translocator protein (TSPO) ligands. Bioorganic & medicinal chemistry 20120915
The expression of translocator protein in human thyroid cancer and its role in the response of thyroid cancer cells to oxidative stress. The Journal of endocrinology 20120801
Effects of minocycline on endogenous neural stem cells after experimental stroke. Neuroscience 20120726
The nitric oxide donor sodium nitroprusside requires the 18 kDa Translocator Protein to induce cell death. Apoptosis : an international journal on programmed cell death 20120701
The 18 kDa translocator protein influences angiogenesis, as well as aggressiveness, adhesion, migration, and proliferation of glioblastoma cells. Pharmacogenetics and genomics 20120701
Non-invasive anatomic and functional imaging of vascular inflammation and unstable plaque. European heart journal 20120601
Synthesis and biological evaluation of 4-phenylquinazoline-2-carboxamides designed as a novel class of potent ligands of the translocator protein. Journal of medicinal chemistry 20120510
The role of 18 kDa mitochondrial translocator protein (TSPO) in programmed cell death, and effects of steroids on TSPO expression. Current molecular medicine 20120501
Developmental expression of the translocator protein 18 kDa (TSPO) in testicular germ cells. Current molecular medicine 20120501
PK11195 inhibits mitophagy targeting the F1Fo-ATPsynthase in Bcl-2 knock-down cells. Current molecular medicine 20120501
Evidence for complex binding profiles and species differences at the translocator protein (TSPO) (18 kDa). Current molecular medicine 20120501
Imaging microglial/macrophage activation in spinal cords of experimental autoimmune encephalomyelitis rats by positron emission tomography using the mitochondrial 18 kDa translocator protein radioligand [¹⁸F]DPA-714. The Journal of neuroscience : the official journal of the Society for Neuroscience 20120425
Solution structures of the prototypical 18 kDa translocator protein ligand, PK 11195, elucidated with 1H/13C NMR spectroscopy and quantum chemistry. ACS chemical neuroscience 20120418
Role of neurosteroids in the anticonvulsant activity of midazolam. British journal of pharmacology 20120401
Substantia nigra vulnerability after a single moderate diffuse brain injury in the rat. Experimental neurology 20120301
18F-FEAnGA for PET of β-glucuronidase activity in neuroinflammation. Journal of nuclear medicine : official publication, Society of Nuclear Medicine 20120301
Effects of translocator protein (18 kDa) ligands on microglial activation and neuronal death in the quinolinic-acid-injected rat striatum. ACS chemical neuroscience 20120215
PK11195, a specific ligand of the peripheral benzodiazepine receptor, may protect pancreatic beta-cells from cytokine-induced cell death. Artificial cells, blood substitutes, and immobilization biotechnology 20120201
Actions of translocator protein ligands on neutrophil adhesion and motility induced by G-protein coupled receptor signaling. Biochemical and biophysical research communications 20120113
An 18-kDa translocator protein (TSPO) polymorphism explains differences in binding affinity of the PET radioligand PBR28. Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism 20120101
Species-dependent and receptor-selective action of bilobalide on the function of constitutive androstane receptor and pregnane X receptor. Drug metabolism and disposition: the biological fate of chemicals 20120101
Visualising neuroinflammation in post-stroke patients: a comparative PET study with the TSPO molecular imaging biomarkers [11C]PK11195 and [11C]vinpocetine. Current radiopharmaceuticals 20120101
The 18 kDa translocator protein (peripheral benzodiazepine receptor) expression in the bone of normal, osteoprotegerin or low calcium diet treated mice. PloS one 20120101
Acute HCV/HIV coinfection is associated with cognitive dysfunction and cerebral metabolite disturbance, but not increased microglial cell activation. PloS one 20120101
New in vitro tools to study human constitutive androstane receptor (CAR) biology: discovery and comparison of human CAR inverse agonists. Molecular pharmaceutics 20111205
In vitro mitochondrial effects of PK 11195, a synthetic translocator protein 18 kDa (TSPO) ligand, in human osteoblast-like cells. Journal of bioenergetics and biomembranes 20111201
Synthesis and structure-activity relationship studies in translocator protein ligands based on a pyrazolo[3,4-b]quinoline scaffold. Journal of medicinal chemistry 20111027
Synthesis and evaluation of novel carbon-11 labeled oxopurine analogues for positron emission tomography imaging of translocator protein (18 kDa) in peripheral organs. Journal of medicinal chemistry 20110908
Tertiary amides with a five-membered heteroaromatic ring as new probes for the translocator protein. European journal of medicinal chemistry 20110901
Erythrocyte peripheral type benzodiazepine receptor/voltage-dependent anion channels are upregulated by Plasmodium falciparum. Blood 20110825
Synthesis of 6-[¹⁸F]fluoro-PBR28, a novel radiotracer for imaging the TSPO 18 kDa with PET. Bioorganic & medicinal chemistry letters 20110815
N-(4-cyanotetrahydro-2H-pyran-4-yl) and N-(1-cyanocyclohexyl) derivatives of 1,5-diarylpyrazole-3-carboxamides showing high affinity for 18 kDa translocator protein and/or cannabinoid receptors. Journal of medicinal chemistry 20110428
Modulation of constitutive androstane receptor (CAR) and pregnane X receptor (PXR) by 6-arylpyrrolo[2,1-d][1,5]benzothiazepine derivatives, ligands of peripheral benzodiazepine receptor (PBR). Toxicology letters 20110425
Multiparametric assessment of acute and subacute ischemic neuronal damage: a small animal positron emission tomography study with rat photochemically induced thrombosis model. Synapse (New York, N.Y.) 20110301
Translocator protein (18 kDa)/peripheral benzodiazepine receptor specific ligands induce microglia functions consistent with an activated state. Glia 20110201
Neuroinflammation is associated with changes in glial mGluR5 expression and the development of neonatal excitotoxic lesions. Glia 20110201
Melatonin and minocycline for combinatorial therapy to improve functional and histopathological deficits following traumatic brain injury. Neuroscience letters 20110113
Evaluation of novel N1-methyl-2-phenylindol-3-ylglyoxylamides as a new chemotype of 18 kDa translocator protein-selective ligand suitable for the development of positron emission tomography radioligands. Journal of medicinal chemistry 20110113
Progesterone turnover to its 5α-reduced metabolites in the ventral tegmental area of the midbrain is essential for initiating social and affective behavior and progesterone metabolism in female rats. Journal of endocrinological investigation 20110101
Quantitative, preclinical PET of translocator protein expression in glioma using 18F-N-fluoroacetyl-N-(2,5-dimethoxybenzyl)-2-phenoxyaniline. Journal of nuclear medicine : official publication, Society of Nuclear Medicine 20110101
Mixed-affinity binding in humans with 18-kDa translocator protein ligands. Journal of nuclear medicine : official publication, Society of Nuclear Medicine 20110101
Increased cerebral (R)-[(11)C]PK11195 uptake and glutamate release in a rat model of traumatic brain injury: a longitudinal pilot study. Journal of neuroinflammation 20110101
Rational quantitative structure-activity relationship (RQSAR) screen for PXR and CAR isoform-specific nuclear receptor ligands. Chemico-biological interactions 20101205
4'-chlorodiazepam--agonist of peripheral benzodiazepine receptors as a protecting factor in IL-1 induced deregulation of collagen biosynthesis in cultured human chondrocytes. European journal of pharmacology 20101125
Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO). Bioorganic & medicinal chemistry letters 20101001
Decreases in binding capacity of the mitochondrial 18 kda translocator protein accompany oxidative stress and pathological signs in rat liver after DMBA exposure. Toxicologic pathology 20101001
Overexpression of translocator protein in inflammatory bowel disease: potential diagnostic and treatment value. Inflammatory bowel diseases 20100901
Two binding sites for [3H]PBR28 in human brain: implications for TSPO PET imaging of neuroinflammation. Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism 20100901
Imaging of vascular inflammation with [11C]-PK11195 and positron emission tomography/computed tomography angiography. Journal of the American College of Cardiology 20100817
Human dosimetry of carbon-11 labeled N-butan-2-yl-1-(2-chlorophenyl)-N-methylisoquinoline-3-carboxamide extrapolated from whole-body distribution kinetics and radiometabolism in rats. Molecular imaging and biology : MIB : the official publication of the Academy of Molecular Imaging 20100801
In vivo binding of protoporphyrin IX to rat translocator protein imaged with positron emission tomography. Synapse (New York, N.Y.) 20100801
18F-FEAC and 18F-FEDAC: PET of the monkey brain and imaging of translocator protein (18 kDa) in the infarcted rat brain. Journal of nuclear medicine : official publication, Society of Nuclear Medicine 20100801
A consecutive three alanine residue insertion mutant of human CAR: a novel CAR ligand screening system in HepG2 cells. The Journal of toxicological sciences 20100801
Antiproliferative effect of peripheral benzodiazepine receptor antagonist PK11195 in rat mammary tumor cells. Molecular and cellular biochemistry 20100701
Ca 2+ -dependent autophagy is enhanced by the pharmacological agent PK11195. Autophagy 20100701
PK11195 might selectively suppress the quinolinic acid-induced enhancement of anaerobic glycolysis in glial cells. Brain research 20100622
Evaluation of translocator protein quantification as a tool for characterising macrophage burden in human carotid atherosclerosis. Atherosclerosis 20100601
Suppressive effect of diazepam on IFN-gamma production by human T cells. International immunopharmacology 20100301
Comparison of [(11)C]-(R)-PK 11195 and [(11)C]PBR28, two radioligands for translocator protein (18 kDa) in human and monkey: Implications for positron emission tomographic imaging of this inflammation biomarker. NeuroImage 20100215
Ethanol induction of steroidogenesis in rat adrenal and brain is dependent upon pituitary ACTH release and de novo adrenal StAR synthesis. Journal of neurochemistry 20100201
New iodinated quinoline-2-carboxamides for SPECT imaging of the translocator protein. Bioorganic & medicinal chemistry letters 20100201
Translocator protein (18 kDa) mediates the pro-growth effects of diazepam on Ehrlich tumor cells in vivo. European journal of pharmacology 20100125
Minocycline 1-year therapy in multiple-system-atrophy: effect on clinical symptoms and [(11)C] (R)-PK11195 PET (MEMSA-trial). Movement disorders : official journal of the Movement Disorder Society 20100115
[11C]-PK11195 PET: quantification of neuroinflammation and a monitor of anti-inflammatory treatment in Parkinson's disease? Parkinsonism & related disorders 20100101
PK11195 enhances chemosensitivity to cisplatin and paclitaxel in human endometrial and ovarian cancer cells. International journal of molecular medicine 20100101
PET-derived biodistribution and dosimetry of the benzodiazepine receptor-binding radioligand (11)C-(R)-PK11195 in children and adults. Journal of nuclear medicine : official publication, Society of Nuclear Medicine 20100101
Translocator protein (18 kDa) is involved in primitive erythropoiesis in zebrafish. FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20091201
[Radiosynthesis of peripheral benzodiazepine receptor radioligand [N-methyl-(11)C]PK 11195 as an imaging agent for positron emission tomography]. Nan fang yi ke da xue xue bao = Journal of Southern Medical University 20091201
Multimodal microglia imaging of fiber tracts in acute subcortical stroke. Annals of neurology 20091201
Neuroinflammation in the living brain of Parkinson's disease. Parkinsonism & related disorders 20091201
[11C]-DPA-713 and [18F]-DPA-714 as new PET tracers for TSPO: a comparison with [11C]-(R)-PK11195 in a rat model of herpes encephalitis. Molecular imaging and biology : MIB : the official publication of the Academy of Molecular Imaging 20091101
[Imaging of brain microgliosis by PET]. Rinsho shinkeigaku = Clinical neurology 20091101
Intra-cornu ammonis 1 administration of the human immunodeficiency virus-1 protein trans-activator of transcription exacerbates the ethanol withdrawal syndrome in rodents and activates N-methyl-D-aspartate glutamate receptors to produce persisting spatial learning deficits. Neuroscience 20091020
Imaging of peripheral-type benzodiazepine receptor in tumor: in vitro binding and in vivo biodistribution of N-benzyl-N-[(11)C]methyl-2-(7-methyl-8-oxo-2-phenyl-7,8-dihydro-9H-purin-9-yl)acetamide. Nuclear medicine and biology 20091001
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. Nature chemical biology 20091001
Translocator protein blockade reduces prostate tumor growth. Clinical cancer research : an official journal of the American Association for Cancer Research 20091001
Positron emission tomography imaging of neuroinflammation. Journal of child neurology 20090901
Distribution, pharmacological characterization and function of the 18 kDa translocator protein in rat small intestine. Biology of the cell 20090731
Translocator protein (18 kD) as target for anxiolytics without benzodiazepine-like side effects. Science (New York, N.Y.) 20090724
CoCl(2) induces apoptosis via the 18 kDa translocator protein in U118MG human glioblastoma cells. Biochemistry 20090602
Neuroinflammation extends brain tissue at risk to vital peri-infarct tissue: a double tracer [11C]PK11195- and [18F]FDG-PET study. Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism 20090601
Peripheral-type benzodiazepine receptor antagonist is effective in relieving neuropathic pain in mice. Journal of pharmacological sciences 20090501
Quantification of (R)-[11C]PK11195 binding in rheumatoid arthritis. European journal of nuclear medicine and molecular imaging 20090401
Whole-body distribution and metabolism of [N-methyl-11C](R)-1-(2-chlorophenyl)-N-(1-methylpropyl)-3-isoquinolinecarboxamide in humans; an imaging agent for in vivo assessment of peripheral benzodiazepine receptor activity with positron emission tomography. European journal of nuclear medicine and molecular imaging 20090401
Autoradiographical imaging of PPARgamma agonist effects on PBR/TSPO binding in TASTPM mice. Experimental neurology 20090401
Monitoring disease evolution and treatment response in lysosomal disorders by the peripheral benzodiazepine receptor ligand PK11195. Neurobiology of disease 20090401
[18F]FEAC and [18F]FEDAC: Two novel positron emission tomography ligands for peripheral-type benzodiazepine receptor in the brain. Bioorganic & medicinal chemistry letters 20090315
The effects of 3-methylclonazepam on Schistosoma mansoni musculature are not mediated by benzodiazepine receptors. European journal of pharmacology 20090315
Image-derived input functions for PET brain studies. European journal of nuclear medicine and molecular imaging 20090301
Comparative evaluation of the translocator protein radioligands 11C-DPA-713, 18F-DPA-714, and 11C-PK11195 in a rat model of acute neuroinflammation. Journal of nuclear medicine : official publication, Society of Nuclear Medicine 20090301
The translocator protein (18 kDa): central nervous system disease and drug design. Journal of medicinal chemistry 20090212
Molecular imaging reveals unique degenerative changes in experimental glaucoma. Neuroreport 20090128
Microglial activation and amyloid deposition in mild cognitive impairment: a PET study. Neurology 20090106
Uptake of inflammatory cell marker [11C]PK11195 into mouse atherosclerotic plaques. European journal of nuclear medicine and molecular imaging 20090101
Increasing 3alpha,5alpha-THP following inhibition of neurosteroid biosynthesis in the ventral tegmental area reinstates anti-anxiety, social, and sexual behavior of naturally receptive rats. Reproduction (Cambridge, England) 20090101
Carbon 11-labeled Pittsburgh Compound B and carbon 11-labeled (R)-PK11195 positron emission tomographic imaging in Alzheimer disease. Archives of neurology 20090101
Bacterial ortholog of mammalian translocator protein (TSPO) with virulence regulating activity. PloS one 20090101
Evaluation of CLINDE as potent translocator protein (18 kDa) SPECT radiotracer reflecting the degree of neuroinflammation in a rat model of microglial activation. European journal of nuclear medicine and molecular imaging 20081201
Microglia, amyloid, and cognition in Alzheimer's disease: An [11C](R)PK11195-PET and [11C]PIB-PET study. Neurobiology of disease 20081201
Neuroprotective effect of Ro5-4864 following brain injury. Experimental neurology 20081201
Effects of Vinpocetine on mitochondrial function and neuroprotection in primary cortical neurons. Neurochemistry international 20081201
Modulation of intracellular Ca2+ signalling in HeLa cells by the apoptotic cell death enhancer PK11195. Biochemical pharmacology 20081201
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. Journal of medicinal chemistry 20081127
Exploratory, anti-anxiety, social, and sexual behaviors of rats in behavioral estrus is attenuated with inhibition of 3alpha,5alpha-THP formation in the midbrain ventral tegmental area. Behavioural brain research 20081121
2-Phenyl-imidazo[1,2-a]pyridine compounds containing hydrophilic groups as potent and selective ligands for peripheral benzodiazepine receptors: synthesis, binding affinity and electrophysiological studies. Journal of medicinal chemistry 20081113
Increased peripheral benzodiazepine receptors in arterial plaque of patients with atherosclerosis: an autoradiographic study with [(3)H]PK 11195. Atherosclerosis 20081101
Hypothalamic involvement in Huntington's disease: an in vivo PET study. Brain : a journal of neurology 20081101
Noninvasive imaging of macrophages in rheumatoid synovitis using 11C-(R)-PK11195 and positron emission tomography. Arthritis and rheumatism 20081101
The positron emission tomography ligand DAA1106 binds with high affinity to activated microglia in human neurological disorders. Journal of neuropathology and experimental neurology 20081001
Anxiolytic-like effects of N,N-dialkyl-2-phenylindol-3-ylglyoxylamides by modulation of translocator protein promoting neurosteroid biosynthesis. Journal of medicinal chemistry 20080925
Inflammation-induced shift in the valence of spinal GABA-A receptor-mediated modulation of nociception in the adult rat. The journal of pain : official journal of the American Pain Society 20080801
The peripheral benzodiazepine receptor ligand 1-(2-chlorophenyl-methylpropyl)-3-isoquinoline-carboxamide is a novel antagonist of human constitutive androstane receptor. Molecular pharmacology 20080801
Novel reference region model reveals increased microglial and reduced vascular binding of 11C-(R)-PK11195 in patients with Alzheimer's disease. Journal of nuclear medicine : official publication, Society of Nuclear Medicine 20080801
Effect of translocator protein (18 kDa)-ligand binding on neurotransmitter-induced salivary secretion in rat submandibular glands. Biology of the cell 20080701
Rapid and efficient radiosynthesis of [123I]I-PK11195, a single photon emission computed tomography tracer for peripheral benzodiazepine receptors. Nuclear medicine and biology 20080701
Effects of topiramate on seizure susceptibility in kainate-kindled rats: involvement of peripheral-type benzodiazepine receptors. Seizure 20080601
Behavioral effects of dietary cholesterol in rats tested in experimental models of mild stress and cognition tasks. European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology 20080601
Effects of long-term low-dose hormone replacement therapy on the binding capacity of platelet peripheral-type benzodiazepine receptor in postmenopausal women. Psychoneuroendocrinology 20080601
Synthesis, fluorine-18 radiolabeling, and in vitro characterization of 1-iodophenyl-N-methyl-N-fluoroalkyl-3-isoquinoline carboxamide derivatives as potential PET radioligands for imaging peripheral benzodiazepine receptor. Bioorganic & medicinal chemistry 20080601
Epilepsy surgery in a case of encephalitis: use of 11C-PK11195 positron emission tomography. Pediatric neurology 20080601
In vivo imaging of microglial activation using a peripheral benzodiazepine receptor ligand: [11C]PK-11195 and animal PET following ethanol injury in rat striatum. Annals of nuclear medicine 20080601
Methamphetamine causes microglial activation in the brains of human abusers. The Journal of neuroscience : the official journal of the Society for Neuroscience 20080528
Investigation of the anticonvulsive effect of acute immobilization stress in anxious Balb/cByJ mice using GABA A-related mechanistic probes. Psychopharmacology 20080501
VMAT2 and dopamine neuron loss in a primate model of Parkinson's disease. Journal of neurochemistry 20080401
Quinolinic acid induced neurodegeneration in the striatum: a combined in vivo and in vitro analysis of receptor changes and microglia activation. European journal of nuclear medicine and molecular imaging 20080401
Effect of PK11195 on attenuating the enhancement of glucose utilization induced by quinolinic acid infusion in the rat brain. Synapse (New York, N.Y.) 20080401
PET image denoising using a synergistic multiresolution analysis of structural (MRI/CT) and functional datasets. Journal of nuclear medicine : official publication, Society of Nuclear Medicine 20080401
Radiosynthesis and in vivo evaluation of N-[11C]methylated imidazopyridineacetamides as PET tracers for peripheral benzodiazepine receptors. Nuclear medicine and biology 20080401
Synthesis and structure-activity relationship studies in peripheral benzodiazepine receptor ligands related to alpidem. Bioorganic & medicinal chemistry 20080315
Comparative anticancer effects of flavonoids and diazepam in cultured cancer cells. Biological & pharmaceutical bulletin 20080201
Ro5-4864 promotes neonatal motor neuron survival and nerve regeneration in adult rats. The European journal of neuroscience 20080201
A comparison of the physiological, behavioral, neurochemical and microglial effects of methamphetamine and 3,4-methylenedioxymethamphetamine in the mouse. Neuroscience 20080124
Functional neuroimaging in multiple sclerosis with radiolabelled glia markers: preliminary comparative PET studies with [11C]vinpocetine and [11C]PK11195 in patients. Journal of the neurological sciences 20080115
The influence of clozapine treatment and other antipsychotics on the 18 kDa translocator protein, formerly named the peripheral-type benzodiazepine receptor, and steroid production. European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology 20080101
Steroidogenesis in BeWo cells: role of protein kinase A and benzodiazepines. The international journal of biochemistry & cell biology 20080101
Ligands of the mitochondrial 18 kDa translocator protein attenuate apoptosis of human glioblastoma cells exposed to erucylphosphohomocholine. Cellular oncology : the official journal of the International Society for Cellular Oncology 20080101
The neurosteroid system: an emerging therapeutic target for hepatic encephalopathy. Metabolic brain disease 20071201
Radiation dosimetry and biodistribution in monkey and man of 11C-PBR28: a PET radioligand to image inflammation. Journal of nuclear medicine : official publication, Society of Nuclear Medicine 20071201
The potential anticancer agent PK11195 induces apoptosis irrespective of p53 and ATM status in chronic lymphocytic leukemia cells. Haematologica 20071201
In vitro and ex vivo autoradiography studies on peripheral-type benzodiazepine receptor binding using [11C]AC-5216 in normal and kainic acid-lesioned rats. Neuroscience letters 20071127
Translocator protein (18 kDa) ligand PK 11195 induces transient mitochondrial Ca2+ release leading to transepithelial Cl- secretion in HT-29 human colon cancer cells. Biology of the cell 20071101
In vivo imaging of brain lesions with [(11)C]CLINME, a new PET radioligand of peripheral benzodiazepine receptors. Glia 20071101
Activated macrophages in HIV encephalitis and a macaque model show increased [3H](R)-PK11195 binding in a PI3-kinase-dependent manner. Neuroscience letters 20071016
Quantifying the A1AR distribution in peritumoural zones around experimental F98 and C6 rat brain tumours. Journal of neuro-oncology 20071001
The lack of expression of the peripheral benzodiazepine receptor characterises microglial response in anaplastic astrocytomas. Journal of neuro-oncology 20071001
A comparison of the high-affinity peripheral benzodiazepine receptor ligands DAA1106 and (R)-PK11195 in rat models of neuroinflammation: implications for PET imaging of microglial activation. Journal of neurochemistry 20070901
The high affinity peripheral benzodiazepine receptor ligand DAA1106 binds specifically to microglia in a rat model of traumatic brain injury: implications for PET imaging. Experimental neurology 20070901
PKC activation sets an upper limit to the functional plasticity of GABAergic transmission induced by endogenous neurosteroids. The European journal of neuroscience 20070901
Intracellular cholesterol changes induced by translocator protein (18 kDa) TSPO/PBR ligands. Neuropharmacology 20070801
Pharmacological characterization of the receptor mediating the anorexigenic action of the octadecaneuropeptide: evidence for an endozepinergic tone regulating food intake. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology 20070701
Characterization of two classes of benzodiazepine binding sites in Schistosoma mansoni. Parasitology 20070701
Microglial activation in presymptomatic Huntington's disease gene carriers. Brain : a journal of neurology 20070701
Peripheral-type benzodiazepine receptors in bronchoalveolar lavage cells of patients with interstitial lung disease. Nuclear medicine and biology 20070701
Positron emission tomography imaging of neuroinflammation. Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics 20070701
Microglial activation in perinatal rabbit brain induced by intrauterine inflammation: detection with 11C-(R)-PK11195 and small-animal PET. Journal of nuclear medicine : official publication, Society of Nuclear Medicine 20070601
A systematic comparison of kinetic modelling methods generating parametric maps for [(11)C]-(R)-PK11195. NeuroImage 20070515
Imaging microglial activation in Huntington's disease. Brain research bulletin 20070430
Peripheral benzodiazepine receptor ligand, PK11195 induces mitochondria cytochrome c release and dissipation of mitochondria potential via induction of mitochondria permeability transition. European journal of pharmacology 20070410
Peripheral-type benzodiazepine receptor (PBR) aggregation and absence of steroidogenic acute regulatory protein (StAR)/PBR association in the mitochondrial membrane as determined by bioluminescence resonance energy transfer (BRET). The Journal of steroid biochemistry and molecular biology 20070401
11C-DPA-713: a novel peripheral benzodiazepine receptor PET ligand for in vivo imaging of neuroinflammation. Journal of nuclear medicine : official publication, Society of Nuclear Medicine 20070401
Targeted imaging of colonic tumors in smad3-/- mice discriminates cancer and inflammation. Molecular cancer research : MCR 20070401
Inhibition of the mitochondrial F1F0-ATPase by ligands of the peripheral benzodiazepine receptor. Bioorganic & medicinal chemistry letters 20070315
N-(5-Fluoro-2-phenoxyphenyl)-N-(2-[(131)I]iodo-5-me thoxybenzyl)acetamide: a potent iodinated radioligand for the peripheral-type benzodiazepine receptor in brain. Journal of medicinal chemistry 20070222
Reprogramming of genetic networks during initiation of the Fetal Alcohol Syndrome. Developmental dynamics : an official publication of the American Association of Anatomists 20070201
New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation. Journal of medicinal chemistry 20070125
PET imaging with [11C]PBR28 can localize and quantify upregulated peripheral benzodiazepine receptors associated with cerebral ischemia in rat. Neuroscience letters 20070116
Channel-like functions of the 18-kDa translocator protein (TSPO): regulation of apoptosis and steroidogenesis as part of the host-defense response. Current pharmaceutical design 20070101
Effects of peripheral-type benzodiazepine receptor ligands on Ehrlich tumor cell proliferation. European journal of pharmacology 20061121
Blood flow dependence of the intratumoral distribution of peripheral benzodiazepine receptor binding in intact mouse fibrosarcoma. Nuclear medicine and biology 20061101
Discovery of antiglioma activity of biaryl 1,2,3,4-tetrahydroisoquinoline derivatives and conformationally flexible analogues. Journal of medicinal chemistry 20060921
Peripheral benzodiazepine receptors on platelets of fibromyalgic patients. Clinical biochemistry 20060901
Nuclear imaging of inflammation in neurologic and psychiatric disorders. Current clinical pharmacology 20060901
Resveratrol-induced apoptosis is enhanced in acute lymphoblastic leukemia cells by modulation of the mitochondrial permeability transition pore. Cancer letters 20060818
Effects of D-galactose on the expression of hippocampal peripheral-type benzodiazepine receptor and spatial memory performances in rats. Psychoneuroendocrinology 20060801
Up-regulation of PK11195 binding in areas of axonal degeneration coincides with early microglial activation in mouse brain. The European journal of neuroscience 20060801
The apparent positive cooperativity of in vivo [3H]PK-11195 binding in mouse fibrosarcoma. Nuclear medicine and biology 20060801
Positron emission tomography imaging of peripheral benzodiazepine receptor binding in human immunodeficiency virus-infected subjects with and without cognitive impairment. Journal of neurovirology 20060801
Peripheral benzodiazepine receptors in the brain of cirrhosis patients with manifest hepatic encephalopathy. European journal of nuclear medicine and molecular imaging 20060701
Intrinsic activated microglia map to the peri-infarct zone in the subacute phase of ischemic stroke. Stroke 20060701
Synthesis, labeling, and biological evaluation of halogenated 2-quinolinecarboxamides as potential radioligands for the visualization of peripheral benzodiazepine receptors. Bioorganic & medicinal chemistry 20060615
Synthesis and in vitro binding of N,N-dialkyl-2-phenylindol-3-yl-glyoxylamides for the peripheral benzodiazepine binding sites. Bioorganic & medicinal chemistry 20060601
Imaging the peripheral benzodiazepine receptor response in central nervous system demyelination and remyelination. Toxicological sciences : an official journal of the Society of Toxicology 20060601
5-aryl-imidazo[2,1-c][1,4]benzodiazepine derivatives as tricyclic constrained analogues of diazepam and Ro5-4864. Synthesis and binding properties at peripheral and central benzodiazepine receptors. Die Pharmazie 20060601
Mitochondrial ligand inhibits store-operated calcium influx and COX-2 production in human microglia. Journal of neuroscience research 20060515
[2-11C]isopropyl-, [1-11C]ethyl-, and [11C]methyl-labeled phenoxyphenyl acetamide derivatives as positron emission tomography ligands for the peripheral benzodiazepine receptor: radiosynthesis, uptake, and in vivo binding in brain. Journal of medicinal chemistry 20060504
Microsphere-based protease assays and screening application for lethal factor and factor Xa. Cytometry. Part A : the journal of the International Society for Analytical Cytology 20060501
Interaction of novel condensed triazine derivatives with central and peripheral type benzodiazepine receptors: synthesis, in vitro pharmacology and modelling. European journal of medicinal chemistry 20060401
The effects of prostaglandin F2alpha treatment on peripheral-type benzodiazepine receptors in the ovary and uterus during pseudopregnancy of rats. Biochemical pharmacology 20060214
In vivo imaging of microglial activation with [11C](R)-PK11195 PET in idiopathic Parkinson's disease. Neurobiology of disease 20060201
[Imaging of glial cells by positron-emitted peripheral benzodiazepine receptor ligands]. Nihon shinkei seishin yakurigaku zasshi = Japanese journal of psychopharmacology 20060201
In vivo imaging of microglial activation with [11C](R)-PK11195 PET in progressive supranuclear palsy. Movement disorders : official journal of the Movement Disorder Society 20060101
Peripheral benzodiazepine receptor: characterization in human T-lymphoma Jurkat cells. Molecular pharmacology 20060101
COX-2, CB2 and P2X7-immunoreactivities are increased in activated microglial cells/macrophages of multiple sclerosis and amyotrophic lateral sclerosis spinal cord. BMC neurology 20060101
A peripheral benzodiazepine receptor targeted agent for in vitro imaging and screening. Bioconjugate chemistry 20060101
Antimitotic activity of high affinity ligands for peripheral benzodiazepine receptor (PBR) in some normal and neoplastic cell lines. Advances in medical sciences 20060101
The anxiolytic etifoxine activates the peripheral benzodiazepine receptor and increases the neurosteroid levels in rat brain. Pharmacology, biochemistry, and behavior 20051201
PK11195 potently sensitizes to apoptosis induction independently from the peripheral benzodiazepin receptor. Oncogene 20051117
PK11195, a peripheral benzodiazepine receptor (pBR) ligand, broadly blocks drug efflux to chemosensitize leukemia and myeloma cells by a pBR-independent, direct transporter-modulating mechanism. Blood 20051115
Decreased density of peripheral benzodiazepine receptors in psychiatric patients after a suicide attempt. Life sciences 20051112
Peripheral benzodiazepine receptor ligand PK11195 reduces microglial activation and neuronal death in quinolinic acid-injected rat striatum. Neurobiology of disease 20051101
Methyllycaconitine prevents methamphetamine-induced effects in mouse striatum: involvement of alpha7 nicotinic receptors. The Journal of pharmacology and experimental therapeutics 20051101
Role of the peripheral benzodiazepine receptor in sensory neuron regeneration. Molecular and cellular neurosciences 20051001
A novel carbohydrate-based therapeutic GCS-100 overcomes bortezomib resistance and enhances dexamethasone-induced apoptosis in multiple myeloma cells. Cancer research 20050915
High-affinity peripheral benzodiazepine receptor ligand, PK11195, regulates protein phosphorylation in rat brain mitochondria under control of Ca(2+). Journal of neurochemistry 20050801
Imaging glial cell activation with [11C]-R-PK11195 in patients with AIDS. Journal of neurovirology 20050801
Mechanisms of mitochondrial apoptosis induced by peripheral benzodiazepine receptor ligands in human colorectal cancer cells. Biochemical and biophysical research communications 20050708
Development of a tracer kinetic plasma input model for (R)-[11C]PK11195 brain studies. Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism 20050701
Methyl pyropheophorbide-a analogues: potential fluorescent probes for the peripheral-type benzodiazepine receptor. Effect of central metal in photosensitizing efficacy. Journal of medicinal chemistry 20050602
Novel anellated pyrazoloquinolin-3-ones: synthesis and in vitro BZR activity. Bioorganic & medicinal chemistry 20050516
Structure of the Mg-chelatase cofactor GUN4 reveals a novel hand-shaped fold for porphyrin binding. PLoS biology 20050501
Effect of PK11195, a peripheral benzodiazepine receptor agonist, on insulinoma cell death and insulin secretion. Apoptosis : an international journal on programmed cell death 20050501
Nuclear location-dependent role of peripheral benzodiazepine receptor (PBR) in hepatic tumoral cell lines proliferation. Life sciences 20050415
Ro5-4864, a peripheral benzodiazepine receptor ligand, reduces reactive gliosis and protects hippocampal hilar neurons from kainic acid excitotoxicity. Journal of neuroscience research 20050401
Benzodiazepine receptor-dependent modulation of neutrophil (PMN) free amino- and alpha-keto acid profiles or immune functions. Amino acids 20050201
1-(Phenyl)isoquinoline carboxamides: a novel class of subtype selective inhibitors of thyrotropin-releasing hormone (TRH) receptors. Bioorganic & medicinal chemistry letters 20050201
Structure-activity relationships and effects on neuroactive steroid synthesis in a series of 2-phenylimidazo[1,2-a]pyridineacetamide peripheral benzodiazepine receptors ligands. Journal of medicinal chemistry 20050113
Evidence in favour of a role for peripheral-type benzodiazepine receptor ligands in amplification of neuronal apoptosis. Apoptosis : an international journal on programmed cell death 20050101
Minocycline treatment attenuates microglia activation and non-angiotensin II [125I] CGP42112 binding in brainstem following nodose ganglionectomy. Neuroscience 20050101
In vivo detection of microglial activation in frontotemporal dementia. Annals of neurology 20041201
Response characteristics of the mitochondrial DNA genome in developmental health and disease. Birth defects research. Part C, Embryo today : reviews 20041201
Lack of evidence of direct mitochondrial involvement in the neuroprotective effect of minocycline. European journal of pharmacology 20041128
Peripheral benzodiazepine receptor ligands induce apoptosis and cell cycle arrest in human hepatocellular carcinoma cells and enhance chemosensitivity to paclitaxel, docetaxel, doxorubicin and the Bcl-2 inhibitor HA14-1. Journal of hepatology 20041101
Targeting mitochondria to overcome conventional and bortezomib/proteasome inhibitor PS-341 resistance in multiple myeloma (MM) cells. Blood 20041015
GABA(A)/central benzodiazepine receptor and peripheral benzodiazepine receptor ligands as inducers of phenobarbital-inducible CYP2B and CYP3A. Biochemical pharmacology 20041001
In vivo imaging of microglial activation with [11C](R)-PK11195 PET in corticobasal degeneration. Movement disorders : official journal of the Movement Disorder Society 20041001
Peripheral type benzodiazepine receptor in human parathyroid glands: up-regulation in adenoma. Journal of endocrinological investigation 20041001
Mitochondria in activated microglia in vitro. Journal of neurocytology 20040901
Axonal injury-dependent induction of the peripheral benzodiazepine receptor in small-diameter adult rat primary sensory neurons. The European journal of neuroscience 20040801
The role of peripheral benzodiazepine receptors on the function and survival of isolated human pancreatic islets. European journal of endocrinology 20040801
Peripheral benzodiazepine receptor ligands: mitochondrial transmembrane potential depolarization and apoptosis induction in rat C6 glioma cells. Biochemical pharmacology 20040701
Imaging of activated microglia with PET and [11C]PK 11195 in corticobasal degeneration. Movement disorders : official journal of the Movement Disorder Society 20040701
Inhibition by miltirone of up-regulation of GABAA receptor alpha4 subunit mRNA by ethanol withdrawal in hippocampal neurons. European journal of pharmacology 20040628
Functional characterization and expression of PBR in rat gastric mucosa: stimulation of chloride secretion by PBR ligands. American journal of physiology. Gastrointestinal and liver physiology 20040601
The peripheral benzodiazepine receptor ligand PK11195 overcomes different resistance mechanisms to sensitize AML cells to gemtuzumab ozogamicin. Blood 20040601
Peripheral benzodiazepine receptor imaging in CNS demyelination: functional implications of anatomical and cellular localization. Brain : a journal of neurology 20040601
3,4-Methylenedioxymethamphetamine increases interleukin-1beta levels and activates microglia in rat brain: studies on the relationship with acute hyperthermia and 5-HT depletion. Journal of neurochemistry 20040601
Peripheral-type benzodiazepine receptor (PBR) and PBR drug ligands in fibroblast and fibrosarcoma cell proliferation: role of ERK, c-Jun and ligand-activated PBR-independent pathways. Biochemical pharmacology 20040515
Evaluation of three quinoline-carboxamide derivatives as potential radioligands for the in vivo pet imaging of neurodegeneration. Neurochemistry international 20040501
Development of a new radioligand, N-(5-fluoro-2-phenoxyphenyl)-N-(2-[18F]fluoroethyl-5-methoxybenzyl)acetamide, for pet imaging of peripheral benzodiazepine receptor in primate brain. Journal of medicinal chemistry 20040422
Antinociceptive effects of peripheral benzodiazepine receptors. Pharmacology 20040401
Attenuation of chronic neuroinflammation by a nitric oxide-releasing derivative of the antioxidant ferulic acid. Journal of neurochemistry 20040401
Evidence of widespread cerebral microglial activation in amyotrophic lateral sclerosis: an [11C](R)-PK11195 positron emission tomography study. Neurobiology of disease 20040401
Involvement of steroids in anti-inflammatory effects of PK11195 in a murine model of pleurisy. Mediators of inflammation 20040401
N,N-dialkyl-2-phenylindol-3-ylglyoxylamides. A new class of potent and selective ligands at the peripheral benzodiazepine receptor. Journal of medicinal chemistry 20040325
In vitro effects of lead ions on peripheral benzodiazepine receptors and adenylyl cyclase activity in the mantle of Mytilus galloprovincialis. Comparative biochemistry and physiology. Toxicology & pharmacology : CBP 20040201
Involvement of steroids in anti-inflammatory effects of peripheral benzodiazepine receptor ligands. Life sciences 20040130
Production of 5alpha-reduced neurosteroids is developmentally regulated and shapes GABA(A) miniature IPSCs in lamina II of the spinal cord. The Journal of neuroscience : the official journal of the Society for Neuroscience 20040128
Effects of peripheral benzodiazepine receptor ligands on proliferation and differentiation of human mesenchymal stem cells. Journal of cellular physiology 20040101
[3H]PK11195 binding sites in human neutrophils: effect of fMLP stimulation and modulation in rheumatic diseases. Clinical biochemistry 20040101
Involvement of benzodiazepine receptors in neuroinflammatory and neurodegenerative diseases: evidence from activated microglial cells in vitro. Neurobiology of disease 20031201
Melanoma differentiation associated gene-7, mda-7/interleukin-24, induces apoptosis in prostate cancer cells by promoting mitochondrial dysfunction and inducing reactive oxygen species. Cancer research 20031201
Increase in peripheral benzodiazepine receptors and loss of glutamate NMDA receptors in a mouse model of closed head injury: a quantitative autoradiographic study. NeuroImage 20031201
Protoporphyrin IX binding and transport by recombinant mouse PBR. Biochemical and biophysical research communications 20031128
Effects of acute and long-term diazepam administrations on neutrophil activity: a flow cytometric study. European journal of pharmacology 20031008
Structure activity studies of a novel cytotoxic benzodiazepine. Bioorganic & medicinal chemistry letters 20031006
Selective neuronal vulnerability following mild focal brain ischemia in the mouse. Brain pathology (Zurich, Switzerland) 20031001
Ligands of the peripheral benzodiazepine receptor have therapeutic effects in pneumopathies in vivo. Immunology letters 20030908
Structure-activity relationships in carboxamide derivatives based on the targeted delivery of radionuclides and boron atoms by means of peripheral benzodiazepine receptor ligands. Journal of medicinal chemistry 20030814
Reversal of Bcl-2-mediated resistance of the EW36 human B-cell lymphoma cell line to arsenite- and pesticide-induced apoptosis by PK11195, a ligand of the mitochondrial benzodiazepine receptor. Toxicological sciences : an official journal of the Society of Toxicology 20030701
Mitochondrial benzodiazepine receptors in the ventral tegmental area modulate sexual behaviour of cycling or hormone-primed hamsters. Journal of neuroendocrinology 20030701
Antidepressant-like effect of Ro5-4864, a peripheral-type benzodiazepine receptor ligand, in forced swimming test. European journal of pharmacology 20030613
Cell-type-specific opening of the retinal ganglion cell mitochondrial permeability transition pore. Investigative ophthalmology & visual science 20030601
PET visualization of microglia in multiple sclerosis patients using [11C]PK11195. European journal of neurology 20030501
Comparison of two PBR ligands with classical antiinflammatory drugs in LPS-induced arthritis in rats. Life sciences 20030425
Neuroprotective effects of (+/-)-huprine Y on in vitro and in vivo models of excitoxicity damage. Experimental neurology 20030401
Benzodiazepine-induced protein tyrosine nitration in rat astrocytes. Hepatology (Baltimore, Md.) 20030201
Peripheral benzodiazepine receptors: on mice and human brain imaging. Journal of neurochemistry 20030201
Elevated peripheral benzodiazepine receptor expression in simian immunodeficiency virus encephalitis. Journal of neurovirology 20030201
The peripheral benzodiazepine receptor ligand PK11195 binds with high affinity to the acute phase reactant alpha1-acid glycoprotein: implications for the use of the ligand as a CNS inflammatory marker. Nuclear medicine and biology 20030201
Exposure-disease continuum for 2-chloro-2'-deoxyadenosine, a prototype ocular teratogen. 3. Intervention with PK11195. Birth defects research. Part A, Clinical and molecular teratology 20030201
[18F]FMDAA1106 and [18F]FEDAA1106: two positron-emitter labeled ligands for peripheral benzodiazepine receptor (PBR). Bioorganic & medicinal chemistry letters 20030120
Involvement of the peripheral benzodiazepine receptor in the development of cutaneous pathology in Mrl/Lpr mice. Immunology letters 20030102
Lordosis of rats is modified by neurosteroidogenic effects of membrane benzodiazepine receptors in the ventral tegmental area. Neuroendocrinology 20030101
Assessment of neuroinflammation and microglial activation in Alzheimer's disease with radiolabelled PK11195 and single photon emission computed tomography. A pilot study. European neurology 20030101
Mitochondrial benzodiazepine receptors regulate oxygen homeostasis in the early mouse embryo. Reproductive toxicology (Elmsford, N.Y.) 20030101
Peripheral benzodiazepine receptor ligand-melphalan conjugates for potential selective drug delivery to brain tumors. Bioconjugate chemistry 20030101
Specific ligands of the peripheral benzodiazepine receptor induce apoptosis and cell cycle arrest in human esophageal cancer cells. International journal of cancer 20021201
Inhibitory effect of diazepam on muscarinic receptor-stimulated inositol 1,4,5-trisphosphate production in rat parotid acinar cells. British journal of pharmacology 20021201
Effects on free radical generation by ligands of the peripheral benzodiazepine receptor in cultured neural cells. Journal of neurochemistry 20021201
Visualising microglial activation in vivo. Glia 20021101
Identification of a peptide antagonist to the peripheral-type benzodiazepine receptor that inhibits hormone-stimulated leydig cell steroid formation. The Journal of pharmacology and experimental therapeutics 20021101
Inhibition of lipopolysaccharide-induced cyclooxygenase-2, tumor necrosis factor-alpha and [Ca2+]i responses in human microglia by the peripheral benzodiazepine receptor ligand PK11195. Journal of neurochemistry 20021101
Regulation of steroid hormone biosynthesis in R2C and MA-10 Leydig tumor cells: role of the cholesterol transfer proteins StAR and PBR. Endocrine research 20021101
Pk11195, a mitochondrial benzodiazepine receptor antagonist, reduces apoptosis threshold in Bcl-X(L) and Mcl-1 expressing human cholangiocarcinoma cells. Gut 20021001
The apoptotic effect of HA14-1, a Bcl-2-interacting small molecular compound, requires Bax translocation and is enhanced by PK11195. Molecular cancer therapeutics 20021001
Involvement of the peripheral benzodiazepine receptor in the development of rheumatoid arthritis in Mrl/lpr mice. European journal of pharmacology 20020927
Synthesis of new molecular probes for investigation of steroid biosynthesis induced by selective interaction with peripheral type benzodiazepine receptors (PBR). Journal of medicinal chemistry 20020912
Apoptosis in activated rat pancreatic stellate cells. American journal of physiology. Gastrointestinal and liver physiology 20020901
Region-selective effects of neuroinflammation and antioxidant treatment on peripheral benzodiazepine receptors and NMDA receptors in the rat brain. Journal of neurochemistry 20020801
Modulation of tamoxifen-induced apoptosis by peripheral benzodiazepine receptor ligands in breast cancer cells. Biochemical pharmacology 20020701
Platelet-activating factor induces permeability transition and cytochrome c release in isolated brain mitochondria. Journal of neuroscience research 20020701
The role of the peripheral benzodiazepine receptor in photodynamic activity of certain pyropheophorbide ether photosensitizers: albumin site II as a surrogate marker for activity. Photochemistry and photobiology 20020701
The peripheral benzodiazepine receptor in photodynamic therapy with the phthalocyanine photosensitizer Pc 4. Photochemistry and photobiology 20020601
Cognitive deficits and CNS damage after a 4-day binge ethanol exposure in rats. Pharmacology, biochemistry, and behavior 20020601
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells. The Journal of biological chemistry 20020419
Effect of diazepam and clonazepam on the function of isolated rat platelet and neutrophil. Medical science monitor : international medical journal of experimental and clinical research 20020401
Peripheral benzodiazepine receptor ligands reverse apoptosis resistance of cancer cells in vitro and in vivo. Cancer research 20020301
Increased expression of 'peripheral-type' benzodiazepine receptors in human temporal lobe epilepsy: implications for PET imaging of hippocampal sclerosis. Metabolic brain disease 20020301
Neuroinflammation of the nigrostriatal pathway during progressive 6-OHDA dopamine degeneration in rats monitored by immunohistochemistry and PET imaging. The European journal of neuroscience 20020301
PK 11195 attenuates kainic acid-induced seizures and alterations in peripheral-type benzodiazepine receptor (PBR) protein components in the rat brain. Journal of neurochemistry 20020301
Sleep deprivation does not affect indices of necrosis or apoptosis in rat brain. The International journal of neuroscience 20020201
PK11195, a peripheral benzodiazepine receptor ligand, chemosensitizes acute myeloid leukemia cells to relevant therapeutic agents by more than one mechanism. Leukemia research 20020101
PK11195, an isoquinoline carboxamide ligand of the mitochondrial benzodiazepine receptor, increased drug uptake and facilitated drug-induced apoptosis in human multidrug-resistant leukemia cells in vitro. Neoplasma 20020101
Binding of [3H]CB 34, a selective ligand for peripheral benzodiazepine receptors, to rat brain membranes. European journal of pharmacology 20011207
Confluence of antianalgesic action of diverse agents through brain interleukin(1beta) in mice. The Journal of pharmacology and experimental therapeutics 20011101
Specific ligands of the peripheral benzodiazepine receptor induce apoptosis and cell cycle arrest in human colorectal cancer cells. British journal of cancer 20011101
Synergistic interaction of diazepam with 3',5'-cyclic adenosine monophosphate-elevating agents on rat aortic rings. European journal of pharmacology 20011005
2-Arylpyrazolo[1,5-a]pyrimidin-3-yl acetamides. New potent and selective peripheral benzodiazepine receptor ligands. Bioorganic & medicinal chemistry 20011001
Hormonal regulation of peripheral benzodiazepine receptor binding properties is mediated by subunit interaction. Biochemistry 20010828
In-vivo measurement of activated microglia in dementia. Lancet (London, England) 20010811
Diazepam increases the hypothalamic-pituitary-adrenocortical (HPA) axis activity by a cyclic AMP-dependent mechanism. British journal of pharmacology 20010801
Targeted delivery of a peripheral benzodiazepine receptor ligand-gemcitabine conjugate to brain tumors in a xenograft model. Cancer chemotherapy and pharmacology 20010801
Pro-apoptotic interactions between XK469 and the peripheral benzodiazepine receptor. Cancer letters 20010726
Diazepam stimulates migration and phagocytosis of human neutrophils: possible contribution of peripheral-type benzodiazepine receptors and intracellular calcium. Pharmacology 20010701
Reversal of reserpine-induced vacuous chewing movements in rats by melatonin: involvement of peripheral benzodiazepine receptors. Brain research 20010615
Structural and functional study of reconstituted peripheral benzodiazepine receptor. Biochemical and biophysical research communications 20010608
Up-regulation of the peripheral-type benzodiazepine receptor expression and [(3)H]PK11195 binding in gerbil hippocampus after transient forebrain ischemia. Journal of neuroscience research 20010601
Normalization of markers for dopamine innervation in striatum of MPTP-lesioned miniature pigs with intrastriatal grafts. Acta neurologica Scandinavica 20010501
Bcl-2 resistant mitochondrial toxicity mediated by the isoquinoline carboxamide PK11195 involves de novo generation of reactive oxygen species. British journal of cancer 20010501
Reduction of acute inflammation in rats by diazepam: role of peripheral benzodiazepine receptors and corticosterone. Immunopharmacology and immunotoxicology 20010501
Melatonin enhances Th2 cell mediated immune responses: lack of sensitivity to reversal by naltrexone or benzodiazepine receptor antagonists. Molecular and cellular biochemistry 20010501
Peripheral type benzodiazepine binding sites as a tool for the detection and quantification of CNS injury. Current protocols in neuroscience 20010501
Mapping and fitting the peripheral benzodiazepine receptor binding site by carboxamide derivatives. Comparison of different approaches to quantitative ligand-receptor interaction modeling. Journal of medicinal chemistry 20010412
Expression of the peripheral-type benzodiazepine receptor and apoptosis induction in hepatic stellate cells. Gastroenterology 20010401
Peripheral-type benzodiazepine receptor ligands: mitochondrial permeability transition induction in rat cardiac tissue. Biochemical pharmacology 20010315
Orphenadrine prevents 3-nitropropionic acid-induced neurotoxicity in vitro and in vivo. British journal of pharmacology 20010201
Negative inotropic effect of diazepam in isolated guinea pig heart. The Journal of veterinary medical science 20010201
Autoradiography with [3H]PK11195 of spinal tract degeneration in amyotrophic lateral sclerosis. Acta neuropathologica 20010201
The pharmacodynamics of PK 11195 in diazepam-dependent male and female rats. Pharmacology, biochemistry, and behavior 20000801
Brain lesions and delayed water maze learning deficits after intracerebroventricular spermine. Brain research 19980727
Intrathecally administered flumazenil and PK 11195 precipitate abstinence syndrome in freely moving diazepam dependent rats. Drug and alcohol dependence 19961211
PK 11195 reduces the brain availability of lindane in rats and the convulsions induced by this neurotoxic agent. Life sciences 19950101
Increased monoamine oxidase B activity in plaque-associated astrocytes of Alzheimer brains revealed by quantitative enzyme radioautography. Neuroscience 19940901
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