OPC-14523 hydrochloride 是一种具有口服活性的 sigma 和 5-HT1A 受体激动剂，对 sigma 受体 (σ1/2 IC50=47/56 nM)、5-HT1A 受体 (IC50=2.3 nM) 和 5-HT 转运体 (IC50=80 nM) 具有高度亲和力。OPC-14523 hydrochloride 显示抗抑郁药样活性。
货号:ajcx32648
CAS:145969-31-9
分子式:C23H29Cl2N3O2
分子量：450.4
溶解度:DMSO : 83.33 mg/mL (185.01 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 hydrochloride shows antidepressant-like activity[1][2].

OPC-14523 hydrochloride inhibits the in vitro reuptake of 3 H-5-HT (IC50=27 nM), but it shows very weak inhibitory activity on 3H-NE and 3H-DA reuptake[1].

OPC-14523 hydrochloride (0.3-100 mg/kg; p.o.; daily for 0, 2, 4, 7 days) produces a marked antidepressant-like effect in the forced swimming test (FST) with rats and mice without affecting the general locomotor activity[1].

参考文献:
[1]. Tottori K, et al. Antidepressant-like responses to the combined sigma and 5-HT1A receptor agonist OPC-14523. Neuropharmacology. 2001;41(8):976-988.
[2]. Bermack JE, et al. Effects of the potential antidepressant OPC-14523 [1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-methoxy-3,4-dihydro-2-quinolinone monomethanesulfonate] a combined sigma and 5-HT1A ligand: modulation of neuronal activity in the dorsal raphe nucleus. J Pharmacol Exp Ther. 2004;310(2):578-583.