| Autor: |
de la Puente-Redondo V; Veterinary Medicine Research & Development, Pfizer Ltd., Sandwich, Kent, UK., Tingley FD 3rd, Schneider RP, Hickman MA |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of veterinary pharmacology and therapeutics [J Vet Pharmacol Ther] 2007 Aug; Vol. 30 (4), pp. 281-7. |
| DOI: |
10.1111/j.1365-2885.2007.00847.x |
| Abstrakt: |
Maropitant is a novel synthetic nonpeptide neurokinin type 1 (NK1) selective receptor antagonist, recently developed for use in the dog as an antiemetic. The in vivo functional activity of maropitant was investigated in the gerbil foot-tapping model, to determine the ability of maropitant to penetrate the central nervous system and inhibit foot-tapping induced by the selective NK1 agonist GR73632. In comparison with CP-122,721, a previously characterized NK1 receptor antagonist, maropitant (1 mg/kg by s.c. injection) was found to inhibit foot-tapping for significantly longer (P < 0.01). Inhibition of foot-tapping by maropitant was 100% at 2 h and approximately 50% at 8 h postdosing. The mean brain:plasma concentration ratio at 8 h post-treatment was 3.59. These data demonstrate the central functional action of maropitant as a selective and potent NK1 receptor antagonist and help to support and explain its clinical potential as a broad-spectrum antiemetic agent. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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