(±)-Epibatidine is an alkaloid that has been found in Ecuadoran poison frog (E. tricolor) skin extracts and an agonist of α4β2 subunit-containing nicotinic acetylcholine receptors (nAChRs; K = 43 pM). It is selective for α4β2 subunit-containing nAChRs over α7 nAChRs (K = 230 nM). (±)-Epibatidine enhances Rb flux in IMR-32 cells (EC = 7 nM) and induces dopamine release from rat striatal slices (EC = 0.4 nM), effects that can be reduced by the nAChR antagonist mecamylamine . In vivo, (±)-epibatidine induces analgesia in the hot plate test and the Straub-tail response in mice (EDs = 0.005 and 0.02 mg/kg, respectively).
(±)-Epibatidine (CMI 545) dihydrochloride is an agonist of nicotinic with potent analgetic activity. (±)-Epibatidine (CMI 545) dihydrochloride is an alkaloid originally characterized from frog skin. (±)-Epibatidine (CMI 545) dihydrochloride have little or no activity at a variety of other central receptors, including opioid receptors, muscarinic receptors, adrenergic receptors, dopamine receptors, serotonin receptors, and gamma-aminobutyric acid receptors.