化合物 T28256
| 中文名称 | 化合物 T28256 |
|---|---|
| 中文同义词 | 化合物 T28256;化合物 OPC-14523 FREE BASE |
| 英文名称 | OPC-14523 |
| 英文同义词 | OPC-14523;1-(3-(4-(3-chlorophenyl)-1-piperazinyl)propyl)-5-methoxy-3,4-dihydro-2-quinolinone;2(1H)-Quinolinone, 1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-3,4-dihydro-5-methoxy-;OPC-14523 free base;VPI 013;VPI013;VPI-013;OPC 14523 free base,OPC14523 free base |
| CAS号 | 145969-30-8 |
| 分子式 | C23H28ClN3O2 |
| 分子量 | 413.94 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 145969-30-8.mol |
| 结构式 |  |
化合物 T28256 性质
OPC-14523 free base 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 free base 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 nM (IC 50 ) |
OPC-14523 free base (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. |