Resinferatoxin, an ultrapotent capsaicin analogue, has anti-emetic properties in the ferret.
Resinferatoxin (100 micrograms/kg, s.c.), the ultrapotent analogue of capsaicin, when given acutely blocked radiation-(200 rads) and copper sulphate (40 mg% 30 ml, p.o.)-induced emesis in ferrets and substantially decreased loperamide (0.5 mg/kg, s.c.)-induced vomiting, without significantly affecting the von Bezold-Jarisch reflex or gag reflex. It also produced a decrease in core temperature as has been reported for capsaicin. The observation that resinferatoxin reduced or blocked emesis induced by both centrally (loperamide) and peripherally (CuSO4, radiation) acting stimuli suggests a novel anti-emetic action that may provide an insight into clinically useful innovative anti-emetics. The mechanism by which resinferatoxin has its anti-emetic effect is at present unknown, although the combination of results from the present study suggest a central site of action involving modulation of release of neurotransmitter, possibly in the nucleus tractus solitarius.
Andrews
P L
PL
Department of Physiology, St George's Hospital Medical School, Tooting, London, U.K.
Bhandari
P
P
D000818:Animals; D000932:Antiemetics / Q000494:pharmacology*; D001522:Behavior, Animal / Q000187:drug effects; D001794:Blood Pressure / Q000187:drug effects; D001831:Body Temperature / Q000187:drug effects; D002211:Capsaicin / Q000031:analogs & derivatives*; D003300:Copper; D019327:Copper Sulfate; D004224:Diterpenes / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D005260:Female; D005289:Ferrets; D005683:Gagging / Q000187:drug effects; D006339:Heart Rate / Q000187:drug effects; D008139:Loperamide; D008297:Male; D011832:Radiation Injuries / Q000517:prevention & control; D012018:Reflex / Q000187:drug effects; D012119:Respiration / Q000187:drug effects; D014839:Vomiting / Q000139:chemically induced / Q000517:prevention & control
D000932:Antiemetics; D004224:Diterpenes; D008139:Loperamide; D003300:Copper; C024353:resiniferatoxin; D019327:Copper Sulfate; D002211:Capsaicin