(+-)-Epibatidine (hydrochloride)

(+-)-Epibatidine is an alkaloid that has been found in Ecuadoran poison frog (E. tricolor) skin extracts and an agonist of a4B2 subunit-containing nicotinic acetylcholine receptors (nAChRs; Ki = 43 pM).{52706,52707} It is selective for a4B2 subunit-containing nAChRs over a7 nAChRs (Ki = 230 nM).{52706} (+-)-Epibatidine enhances 86Rb+ flux in IMR-32 cells (EC50 = 7 nM) and induces dopamine release from rat striatal slices (EC50 = 0.4 nM), effects that can be reduced by the nAChR antagonist mecamylamine (Item No. 14602). In vivo, (+-)-epibatidine induces analgesia in the hot plate test and the Straub-tail response in mice (ED50s = 0.005 and 0.02 mg/kg, respectively).{52707}