OPC-14523盐酸盐

生物活性靶点体外研究体内研究 OPC-14523盐酸盐试剂级价格

OPC-14523盐酸盐

CAS号:145969-31-9
英文名:Opc-14523 monohcl
中文名:OPC-14523盐酸盐
CBNumber:CB13112619
分子式:C23H29Cl2N3O2
分子量:450.4
MOL File:145969-31-9.mol

OPC-14523盐酸盐化学性质

储存条件 :Store at -20°C
溶解度 :DMSO : 83.33 mg/mL (185.01 mM)
形态 :Solid
颜色 :White to off-white

OPC-14523盐酸盐性质、用途与生产工艺

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.