Tebanicline (hydrochloride)

Properties

Safety Information

Description

ABT-594 is a potent agonist of neuronal α4β2 subunit-containing nicotinic acetylcholine receptors (nAChRs; K_i = 37 pM in a radioligand binding assay). 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. It also induces hypothermia, seizures, and an increase in blood pressure.