ABT-594 is a potent agonist of neuronal α4β2 subunit-containing nicotinic acetylcholine receptors (nAChRs; K = 37 pM in a radioligand binding assay). It is selective for neuronal nAChRs over neuromuscular α1β1δγ subunit-containing nAChRs (K = 10,000 nM), α, α, and α adrenergic receptors (Ks = 890, 597, and 342 nM, respectively), and 70 other receptors, enzymes, and transporters (Ks = >1,000 nM) in radioligand binding assays. ABT-594 induces [Rb] efflux in K177 cells transfected with human neuronal α4β2 subunit-containing nAChRs (EC = 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.
ABT-594 (hydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. ABT-594 (hydrochloride) inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM.
分子式
C9H11ClN2O.HCl
分子量
235.11
CAS号
203564-54-9
运输条件
Room temperature in continental US; may vary elsewhere.