Epibatidine is a nicotinic analgesic

Eur J Pharmacol. 1993 Dec 21;250(3):R13-4. doi: 10.1016/0014-2999(93)90043-h.

Abstract

Epibatidine, an alkaloid isolated from skin of the poison frog, Epipedobates tricolor, has been shown to be a very potent analgesic with a non-opioid mechanism of action. We found that epibatidine was about 120 times more potent and has longer duration than nicotine in analgesia, which could be antagonized by pretreatment with mecamylamine. Furthermore, epibatidine competed with high affinity (IC50 = 70 pM, Ki = 43 pM) for [3H]cytisine binding in rat brain preparations. These results indicated that the analgesic activity of epibatidine is attributed to its unique property as the most potent nicotinic acetylcholine receptor agonist.

Publication types

  • Comparative Study

MeSH terms

  • Alkaloids / metabolism
  • Analgesics / metabolism
  • Analgesics / pharmacology*
  • Animals
  • Azocines
  • Binding, Competitive
  • Brain / drug effects
  • Brain / metabolism*
  • Bridged Bicyclo Compounds / metabolism
  • Bridged Bicyclo Compounds / pharmacology*
  • Bridged Bicyclo Compounds, Heterocyclic*
  • Drug Interactions
  • Mecamylamine / pharmacology
  • Mice
  • Nicotine / metabolism
  • Nicotine / pharmacology
  • Pyridines / metabolism
  • Pyridines / pharmacology*
  • Quinolizines
  • Rats
  • Receptors, Nicotinic / drug effects*
  • Receptors, Nicotinic / metabolism

Substances

  • Alkaloids
  • Analgesics
  • Azocines
  • Bridged Bicyclo Compounds
  • Bridged Bicyclo Compounds, Heterocyclic
  • Pyridines
  • Quinolizines
  • Receptors, Nicotinic
  • cytisine
  • Mecamylamine
  • Nicotine
  • epibatidine