title: Epibatidine is a nicotinic analgesic.
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.
authors.affiliation: CytoMed, Inc., Cambridge, MA 02139.
authors.forename: C
authors.initials: C
authors.lastname: Qian
authors.forename: T
authors.initials: T
authors.lastname: Li
authors.forename: T Y
authors.initials: TY
authors.lastname: Shen
authors.forename: L
authors.initials: L
authors.lastname: Libertine-Garahan
authors.forename: J
authors.initials: J
authors.lastname: Eckman
authors.forename: T
authors.initials: T
authors.lastname: Biftu
authors.forename: S
authors.initials: S
authors.lastname: Ip
mesh_terms: D000470:Alkaloids / Q000378:metabolism; D000700:Analgesics / Q000378:metabolism / Q000494:pharmacology*; D000818:Animals; D001392:Azocines; D001667:Binding, Competitive; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D001643:Bridged Bicyclo Compounds / Q000378:metabolism / Q000494:pharmacology*; D019086:Bridged Bicyclo Compounds, Heterocyclic; D004347:Drug Interactions; D008464:Mecamylamine / Q000494:pharmacology; D051379:Mice; D009538:Nicotine / Q000378:metabolism / Q000494:pharmacology; D011725:Pyridines / Q000378:metabolism / Q000494:pharmacology*; D011807:Quinolizines; D051381:Rats; D011978:Receptors, Nicotinic / Q000187:drug effects* / Q000378:metabolism; D000093843:Quinolizidine Alkaloids
chemical_list: D000470:Alkaloids; D000700:Analgesics; D001392:Azocines; D001643:Bridged Bicyclo Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; D008464:Mecamylamine; D009538:Nicotine; D011725:Pyridines; D011807:Quinolizines; D011978:Receptors, Nicotinic; C004712:cytisine; D000093843:Quinolizidine Alkaloids; C082748:epibatidine