GR 205171
| Title | Journal |
|---|---|
| A pharmacokinetic PET study of NK₁ receptor occupancy. | European journal of nuclear medicine and molecular imaging 20120201 |
| Discovery and biological characterization of (2R,4S)-1'-acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4,4'-bipiperidine-1-carboxamide as a new potent and selective neurokinin 1 (NK1) receptor antagonist clinical candidate. | Journal of medicinal chemistry 20110224 |
| Potentiation of the anticonvulsant efficacy of sodium channel inhibitors by an NK1-receptor antagonist in the rat. | Epilepsia 20100801 |
| Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist. | Journal of medicinal chemistry 20090528 |
| Inhibition of the bradycardic component of the von Bezold-Jarisch reflex and carotid chemoreceptor reflex by periaqueductal gray stimulation: involvement of medullary receptors. | The European journal of neuroscience 20090501 |
| Neurokinin1 antagonists potentiate antidepressant properties of serotonin reuptake inhibitors, yet blunt their anxiogenic actions: a neurochemical, electrophysiological, and behavioral characterization. | Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology 20090301 |
| Differential effects of dexamethasone, ondansetron and a tachykinin NK1 receptor antagonist (GR205171) on cisplatin-induced changes in behaviour, food intake, pica and gastric function in rats. | European journal of pharmacology 20070126 |
| Synthesis of two potential NK1-receptor ligands using [1-11C]ethyl iodide and [1-11C]propyl iodide and initial PET-imaging. | BMC medical imaging 20070101 |
| A new application of pre-normalized principal component analysis for improvement of image quality and clinical diagnosis in human brain PET studies--clinical brain studies using [11C]-GR205171, [11C]-L-deuterium-deprenyl, [11C]-5-Hydroxy-L-Tryptophan, [11C]-L-DOPA and Pittsburgh Compound-B. | NeuroImage 20061101 |
| Proteomic analysis of rat hippocampus and frontal cortex after chronic treatment with fluoxetine or putative novel antidepressants: CRF1 and NK1 receptor antagonists. | European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology 20061001 |
| Blockade of tachykinin NK1 receptors attenuates stress-induced rise of extracellular noradrenaline and dopamine in the rat and gerbil medial prefrontal cortex. | Journal of neuroscience research 20061001 |
| Antidepressant-like activity of selective serotonin reuptake inhibitors combined with a NK1 receptor antagonist in the mouse forced swimming test. | Behavioural brain research 20060925 |
| [3H]GR205171 displays similar NK1 receptor binding profile in gerbil and human brain. | British journal of pharmacology 20060501 |
| Use of LC/MS to assess brain tracer distribution in preclinical, in vivo receptor occupancy studies: dopamine D2, serotonin 2A and NK-1 receptors as examples. | Life sciences 20051212 |
| Sustained pharmacological blockade of NK1 substance P receptors causes functional desensitization of dorsal raphe 5-HT 1A autoreceptors in mice. | Journal of neurochemistry 20051201 |
| Antidepressant-like effects of agomelatine, melatonin and the NK1 receptor antagonist GR205171 in impulsive-related behaviour in rats. | Psychopharmacology 20051001 |
| TRPV1 activation results in disruption of the blood-brain barrier in the rat. | British journal of pharmacology 20051001 |
| Cerebral blood flow changes after treatment of social phobia with the neurokinin-1 antagonist GR205171, citalopram, or placebo. | Biological psychiatry 20050715 |
| Functional interaction between nucleus tractus solitarius NK1 and 5-HT3 receptors in the inhibition of baroreflex in rats. | Cardiovascular research 20050301 |
| Blockade of substance P (neurokinin 1) receptors enhances extracellular serotonin when combined with a selective serotonin reuptake inhibitor: an in vivo microdialysis study in mice. | Journal of neurochemistry 20040401 |
| Stress-induced increase of cortical dopamine metabolism: attenuation by a tachykinin NK1 receptor antagonist. | European journal of pharmacology 20040119 |
| The new neurokinin 1-sensitive receptor mediates the facilitation by endogenous tachykinins of the NMDA-evoked release of acetylcholine after suppression of dopaminergic transmission in the matrix of the rat striatum. | Journal of neurochemistry 20031001 |
| Contribution of tachykinin receptor subtypes to micturition reflex in guinea pigs. | European journal of pharmacology 20030923 |
| Comparison of the functional blockade of rat substance P (NK1) receptors by GR205171, RP67580, SR140333 and NKP-608. | Neuropharmacology 20030801 |
| Effects of antidepressant drugs and GR 205171, an neurokinin-1 (NK1) receptor antagonist, on the response in the forced swim test and on monoamine extracellular levels in the frontal cortex of the mouse. | Neuroscience letters 20030717 |
| Control by tachykinin NK(2) receptors of CRF(1) receptor-mediated activation of hippocampal acetylcholine release in the rat and guinea-pig. | Neuropeptides 20030401 |
| The selective neurokinin (NK)(1) antagonist, GR205,171, stereospecifically enhances mesocortical dopaminergic transmission in the rat: a combined dialysis and electrophysiological study. | Brain research 20020510 |
| Stereospecific blockade of marble-burying behaviour in mice by selective, non-peptidergic neurokinin1 (NK1) receptor antagonists. | Neuropharmacology 20020401 |
| Permissive role of neurokinin NK(3) receptors in NK(1) receptor-mediated activation of the locus coeruleus revealed by SR 142801. | Synapse (New York, N.Y.) 20020101 |
| Role of tachykinin receptors in the central processing of afferent input from the acid-threatened rat stomach. | Regulatory peptides 20011215 |
| Comparison of the phenotype of NK1R-/- mice with pharmacological blockade of the substance P (NK1 ) receptor in assays for antidepressant and anxiolytic drugs. | Behavioural pharmacology 20011101 |
| Selective blockade of neurokinin (NK)(1) receptors facilitates the activity of adrenergic pathways projecting to frontal cortex and dorsal hippocampus in rats. | Journal of neurochemistry 20010301 |
| Nitric oxide and NK(1)-tachykinin receptors in cyclophosphamide-induced cystitis, in rats. | The Journal of pharmacology and experimental therapeutics 20001101 |
| Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist. | Journal of medicinal chemistry 19981105 |
| GR205171: a novel antagonist with high affinity for the tachykinin NK1 receptor, and potent broad-spectrum anti-emetic activity. | Regulatory peptides 19960827 |