epibatidine

Epibatidine 2HCl is a potent nicotinic agonist.

AT-1001 is an α3β4 nAChR partial agonist. AT-1001 attenuates stress-induced reinstatement of nicotine seeking in a rat model of relapse and induces minimal withdrawal in dependent rats. AT-1001 also potently and reversibly blocks epibatidine-induced inward currents in HEK cells transfected with α3β4 nAChR. Importantly, AT-1001 potently and dose-dependently blocks nicotine self-administration in rats, without affecting food responding. When tested in a nucleus accumbens (NAcs) synaptosomal preparation, AT-1001 inhibits nicotine-induced [³H]dopamine release poorly and at significantly higher concentrations compared with mecamylamine and conotoxin MII.

Epiboxidine, a methylisoxazole analog of the alkaloid Epibatidine and analog of the nAChR agonist ABT 418 [1], serves as a potent and selective agonist for neural nicotinic acetylcholine receptors (nAChR), exhibiting Ki values of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively.

Hemicholinium 3 is a potent and selective choline uptake blocker.

Epiboxidine hydrochloride, a methylisoxazole analog of the alkaloid Epibatidine and an analog of the nAChR agonist ABT 418 [1], serves as a potent and selective agonist of neural nAChRs, demonstrating K i values of 0.46 nM and 1.2 nM for α4β2 nAChRs in rats and humans, respectively.

Tebanicline is a potent synthetic nicotinic (non-opioid) analgesic drug. It was developed as a less toxic analogue of the potent poison dart frog-derived compound epibatidine. Like epibatidine, tebanicline showed potent analgesic activity against neuropat