OPC-14523盐酸盐
| 中文名称 | OPC-14523盐酸盐 |
|---|---|
| 中文同义词 | OPC-14523盐酸盐;化合物 OPC-14523 HYDROCHLORIDE |
| 英文名称 | Opc-14523 monohcl |
| 英文同义词 | Opc-14523 monohcl;1-[3-[4-(3-chlorophenyl)piperazin-1-yl]propyl]-5-methoxy-3,4-dihydroquinolin-2-one;OPC-14523 hydrochloride |
| CAS号 | 145969-31-9 |
| 分子式 | C23H29Cl2N3O2 |
| 分子量 | 450.4 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 145969-31-9.mol |
| 结构式 |  |
OPC-14523盐酸盐 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | 二甲基亚砜：83.33 mg/mL（185.01 mM） |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
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。
|
5-HT 1A Receptor 2.3 nM (IC 50 ) |
sigma 1 47 nM (IC 50 ) |
sigma 2 56 mM (IC 50 ) |
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.
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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-116594A | OPC-14523 hydrochloride | 1 mg | 1590元 | |
| 2024/04/30 | HY-116594A | OPC-14523盐酸盐 OPC-14523 hydrochloride | 145969-31-9 | 5mg | 3500元 |