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 (σ1/2IC50=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。
| 生物活性 | OPC-14523 free base is an orally activesigmaand5-HT1A receptoragonist, with high affinity for sigma receptors (σ1/2IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 free base shows antidepressant-like activity[1][2]. |
| IC50& Target[1] | 5-HT1AReceptor 2.3 nM (IC50) | sigma 1 47 nM (IC50) | sigma 2 56 nM (IC50) |
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体内研究
(In Vivo) | 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[1].
| Animal Model: | Wistar strain of rats (140-245 g)[1] | | 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 ED50value of 27 mg/kg. The ED50value for OPC-14523 on day 7 was 18 mg/kg. |
| Animal Model: | ICR strain of mice (25-45 g)[1] | | 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 ED50value 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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