ABT-594 (hydrochloride)

ABT-594 is a potent agonist of neuronal α4β2 subunit-containing nicotinic acetylcholine receptors (nAChRs; K_i = 37 pM in a radioligand binding assay).¹ It is selective for neuronal nAChRs over neuromuscular α1β1δγ subunit-containing nAChRs (K_i = 10,000 nM), α_1B-, α_2B-, and α_2C- adrenergic receptors (K_is = 890, 597, and 342 nM, respectively), and 70 other receptors, enzymes, and transporters (K_is = >1,000 nM) in radioligand binding assays. ABT-594 induces [⁸⁶Rb⁺] efflux in K177 cells transfected with human neuronal α4β2 subunit-containing nAChRs (EC₅₀ = 140 nM). In vivo, ABT-594 (0.05 and 0.01 mg/kg, s.c.) increases latency to paw withdrawal in a hot-plate test in rats.² It also induces hypothermia, seizures, and an increase in blood pressure.

WARNING This product is not for human or veterinary use.

1. Donnelly-Roberts, D.L., Puttfarcken, P.S., Kuntzweiler, T.A., et al. ABT-594 [(R)-5-(2-azetidinylmethoxy)-2-chloropyridine]: A novel, orally effective analgesic acting via neuronal nicotinic acetylcholine receptors: I. In vitro characterization. J. Pharmacol. Exp. Ther. 285(2), 777-786 (1998).

2. Boyce, S., Webb, J.K., Shepheard, S.L., et al. Analgesic and toxic effects of ABT-594 resemble epibatidine and nicotine in rats. Pain 85(3), 443-450 (2000).