Resinferatoxin, an ultrapotent capsaicin analogue, has anti-emetic properties in the ferret

Neuropharmacology. 1993 Aug;32(8):799-806. doi: 10.1016/0028-3908(93)90189-a.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiemetics / pharmacology*
  • Behavior, Animal / drug effects
  • Blood Pressure / drug effects
  • Body Temperature / drug effects
  • Capsaicin / analogs & derivatives*
  • Copper
  • Copper Sulfate
  • Diterpenes / pharmacology*
  • Dose-Response Relationship, Drug
  • Female
  • Ferrets
  • Gagging / drug effects
  • Heart Rate / drug effects
  • Loperamide
  • Male
  • Radiation Injuries / prevention & control
  • Reflex / drug effects
  • Respiration / drug effects
  • Vomiting / chemically induced
  • Vomiting / prevention & control

Substances

  • Antiemetics
  • Diterpenes
  • Loperamide
  • Copper
  • resiniferatoxin
  • Copper Sulfate
  • Capsaicin