产品
编 号:F616154
分子式:C23H29Cl2N3O2
分子量:450.4
产品类型
结构图
CAS No: 145969-31-9
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产品详情
生物活性:
OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 hydrochloride shows antidepressant-like activity.
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 ED50 value of 27 mg/kg. The ED50 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 ED50 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.
体外研究:
OPC-14523 hydrochloride inhibits the in vitro reuptake of 3 H-5-HT (IC50=27 nM), but it shows very weak inhibitory activity on 3H-NE and 3H-DA reuptake.