145969-31-9
中文名稱
OPC-14523鹽酸鹽
英文名稱
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 結(jié)構(gòu)式
基本信息
中文別名
OPC-14523鹽酸鹽 英文別名
Opc-14523 monohclOPC-14523 hydrochloride
1-[3-[4-(3-chlorophenyl)piperazin-1-yl]propyl]-5-methoxy-3,4-dihydroquinolin-2-one
物理化學(xué)性質(zhì)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO : 83.33 mg/mL (185.01 mM)
形態(tài)Solid
顏色White to off-white
常見問(wèn)題列表
生物活性
OPC-14523 hydrochloride 是一種具有口服活性的 sigma 和 5-HT1A 受體激動(dòng)劑，對(duì) sigma 受體 (σ1/2 IC50=47/56 nM)、5-HT1A 受體 (IC50=2.3 nM) 和 5-HT 轉(zhuǎn)運(yùn)體 (IC50=80 nM) 具有高度親和力。OPC-14523 hydrochloride 顯示抗抑郁藥樣活性。靶點(diǎn)
|
5-HT 1A Receptor 2.3 nM (IC 50 ) |
sigma 1 47 nM (IC 50 ) |
sigma 2 56 mM (IC 50 ) |
體外研究
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.
體內(nèi)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. |