Enantioselective inhibition of apomorphine-induced emesis in the ferret by the neurokinin1 receptor antagonist CP-99,994.
These studies have examined the effects of the selective neurokinin1 (NK1) receptor antagonist CP-99,994 on the retching and vomiting response to apomorphine. CP-99,994 (1-3 mg/kg i.p.) attenuated retching and vomiting induced by apomorphine (0.25 mg/kg s.c.) with complete inhibition of retching and vomiting at the 3 mg/kg dose. In contrast CP-100,263 (3 mg/kg i.p.), the enantiomer of CP-99,994 with 1000-fold lower affinity for the NK1 receptor, was without effect.
Merck, Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, U.K.
F D
FD
Tattersall
W
W
Rycroft
R G
RG
Hill
R J
RJ
Hargreaves
D000818:Animals; D001058:Apomorphine / Q000037:antagonists & inhibitors*; D004305:Dose-Response Relationship, Drug; D005289:Ferrets; D008297:Male; D064729:Neurokinin-1 Receptor Antagonists; D010880:Piperidines / Q000494:pharmacology*; D013237:Stereoisomerism; D014839:Vomiting / Q000139:chemically induced / Q000517:prevention & control*
D064729:Neurokinin-1 Receptor Antagonists; D010880:Piperidines; C080755:3-(2-methoxybenzylamino)-2-phenylpiperidine; D001058:Apomorphine