mdi-book-open-variant Impressum mdi-help Hilfe / Anleitung mdi-printer Webseite ausdrucken mdi-bookmark Bookmark der Webseite speichern mdi-magnify Suche & Index Wirkstoffe mdi-sitemap Sitemap CliniPharm/CliniTox-Webserver mdi-home Startseite CliniPharm/CliniTox-Webserver mdi-email Beratungsdienst: Email / Post / Fax / Telefon

De la Puente-Redondo V, Tingley FD, Schneider RP & Hickman MA
The neurokinin-1 antagonist activity of maropitant, an antiemetic drug for dogs, in a gerbil model.

J Vet Pharmacol Ther, 30(4): 281-287, 2007
ISSN: 0140-7783 Journal of Veterinary Pharmacology and Therapeutics (PubMed)

Abstract
Maropitant is a novel synthetic nonpeptide neurokinin type 1 (NK(1)) 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 NK(1) agonist GR73632. In comparison with CP-122,721, a previously characterized NK(1) 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 NK(1) receptor antagonist and help to support and explain its clinical potential as a broad-spectrum antiemetic agent.

© 2021 - Institut für Veterinärpharmakologie und ‑toxikologie

Es kann keinerlei Haftung für Ansprüche übernommen werden, die aus dieser Webseite erwachsen könnten.