145969-31-9

中文名称 OPC-14523盐酸盐

英文名称 Opc-14523 monohcl

CAS 145969-31-9

分子式 C23H29Cl2N3O2

更新日期 2023/03/20 15:41:21

分子量 450.4

MOL 文件 145969-31-9.mol

145969-31-9 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

OPC-14523盐酸盐

英文别名

Opc-14523 monohcl
OPC-14523 hydrochloride
1-[3-[4-(3-chlorophenyl)piperazin-1-yl]propyl]-5-methoxy-3,4-dihydroquinolin-2-one

物理化学性质

储存条件-20°C储存

溶解度DMSO : 83.33 mg/mL (185.01 mM)

形态Solid

颜色White to off-white

常见问题列表

生物活性

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。

靶点

5-HT _1A Receptor

2.3 nM (IC ₅₀ )

sigma 1

47 nM (IC ₅₀ )

sigma 2

56 mM (IC ₅₀ )

体外研究

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.

体内研究

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.

Animal Model:	Wistar strain of rats (140-245 g)
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)
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.