Epiboxidine hydrochloride

Epiboxidine hydrochloride is a potent and selective neural nAChR agonist with Kis of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. Epiboxidine hydrochloride is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418.

Epiboxidine hydrochloride has affinity and functional at central neuronal α4β2 receptors, with K_is of 0.46 and 1.2 in rat and humen^[1].
Epiboxidine hydrochloride has activity at ganglionic-type α3β4*-nicotinic receptors of PC12 cells, with a K_i of 19^[1].
Epiboxidine hydrochloride is much less toxic than Epibatidine^[1].
Epiboxidine hydrochloride stimulates sodium-22 influx in PC12 and TE671 cells, with EC₅₀s of 0.18 and 2.6 μM^[2].

Epiboxidine hydrochloride (20 μg/kg; ip; once) treatment shows marked analgetic activity in mice^[1].
Epiboxidine hydrochloride (50 and 100 mg/kg; intraperitoneal injected; once) causes marked antinociception as measured in the hot-plate assay^[2].
Epiboxidine hydrochloride inhibits [³H]nicotine binding in rat cerebral cortical membranes, with a K_i of 0.6 nM^[2].

References:
[1]. Fitch RW, et al. Homoepiboxidines: further potent agonists for nicotinic receptors. Bioorg Med Chem. 2004;12(1):179-190.
[2]. Badio B, et al. Synthesis and nicotinic activity of epiboxidine: an isoxazole analogue of epibatidine. Eur J Pharmacol. 1997;321(2):189-194.