vofopitant has been researched along with vestipitant* in 2 studies
1 trial(s) available for vofopitant and vestipitant
| Article | Year |
|---|---|
Anxiolytic effects of vestipitant in a sub-group of healthy volunteers known to be sensitive to CO2 challenge.
The pharmacological properties of two NK1 antagonists were studied in comparison with a benzodiazepine during a 7% CO2 challenge in a population of healthy volunteers selected for a high sensitivity to the challenge. In total, 19 healthy subjects, pre-screened for their responsiveness to the 7% CO2 test, took part in the randomised, double-blind, cross-over, incomplete block design study. After receiving treatment or placebo, the volunteers were subjected to three 7% CO2 challenges each for a time of 20 min. The treatment consisted of the administration of the following three active drugs: a single dose of benzodiazepine alprazolam (0.75 mg) and a single dose of the NK1 antagonists vestipitant (GW597599) (15 mg) and vofopitant (GR205171) (25 mg). Anxiety during the challenge was evaluated with Visual Analogue Scale-Anxiety (VAS-A) and with Panic Symptom List (PSL III-R). Respiratory parameters, heart rate and skin conductance were also recorded. Compared with placebo, vestipitant showed a significant reduction (p<0.05) in anxiety assessed on the VAS-A scale (ΔVAS-A%) while alprazolam significantly (p<0.01) attenuated the PSL III-R total score. Vofopitant did not show any anxiolytic effect. In the comparison analysis between placebo and drugs, none of the respiratory and other physiological parameters showed a statistically significant difference. Topics: Adult; Alprazolam; Anti-Anxiety Agents; Anxiety; Anxiety Disorders; Benzodiazepines; Carbon Dioxide; Cross-Over Studies; Double-Blind Method; Fluorobenzenes; Heart Rate; Humans; Piperidines; Tetrazoles; Young Adult | 2014 |
1 other study(ies) available for vofopitant and vestipitant
| Article | Year |
|---|---|
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.
In an effort to discover novel druglike NK(1) receptor antagonists a new series of suitably substituted C-phenylpiperazine derivatives was identified by an appropriate chemical exploration of related N-phenylpiperazine analogues, with the specific aim to maximize their in vitro affinity and optimize in parallel their pharmacokinetic profile. Among the compounds synthesized, 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) was identified as one of the most in vitro potent and selective NK(1) receptor antagonists ever discovered, showing appropriate pharmacokinetic properties and in vivo activity. On the basis of its preclinical profile, this compound was selected as a drug candidate. Topics: Administration, Oral; Animals; CHO Cells; Cricetinae; Cricetulus; Drug Discovery; Drug Evaluation, Preclinical; Fluorobenzenes; Gerbillinae; Neurokinin-1 Receptor Antagonists; Pharmacokinetics; Piperazines; Piperidines; Structure-Activity Relationship | 2009 |