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 (σ1/2IC50=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。

OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC 50 =47/56 nM), the 5-HT1A receptor ( IC 50 =2.3 nM), and the 5-HT transporter ( IC 50 =80 nM). OPC-14523 hydrochloride shows antidepressant-like activity [1] [2].

OPC-14523 hydrochloride inhibits the in vitro reuptake of 3 H-5-HT (IC 50 =27 nM), but it shows very weak inhibitory activity on 3 H-NE and 3 H-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]. Animal Model: Wistar strain of rats (140-245 g) [1] Dosage: 0.3-100 mg/kg Administration: P.o.; daily for 0, 2, 4, 7 days Result: A single doses of 1 mg/kg and higher of OPC-14523 reduced immobility time in the FST with an ED 50 value of 27 mg/kg. The ED 50 value for OPC-14523 on day 7 was 18 mg/kg. Animal Model: ICR strain of mice (25-45 g) [1] Dosage: 0.3-100 mg/kg Administration: P.o.; daily for 0, 2, 4, 7 days Result: A single oral dose of OPC-14523 produced a marked reduction in immobility time during the FST at oral doses of 1 mg/kg and higher, with an ED 50 value of 20 mg/kg. The potency of OPC-14523 in decreasing immobility time was greater after treatment for seven consecutive days, producing an ED50 value of 2 mg/kg.

145969-31-9

C23H29Cl2N3O2

450.4

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years