Tebanicline (hydrochloride) 化学特性,用途語,生産方法
説明
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 (EC
50 = 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.
Tebanicline (hydrochloride) 上流と下流の製品情報
原材料
準備製品