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编 号:F285067
分子式:C26H39NO10
分子量:525.59
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10mM*1mL in DMSO
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100mg
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500mg
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生物活性:
Pentoxyverine (Carbetapentane) citrate is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membrane σ1, respectively. Pentoxyverine citrate is a muscarinic antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance.

体内研究:
Pentoxyverine (Carbetapentane;1-32mg/kg;皮下给药) citrate 在小鼠的爪子注射辣椒素 (HY-10448) 进行刺激下,可以剂量依赖性地增强辣椒素对机械刺激的敏化作用。Pentoxyverine (16?mg/kg;皮下给药) citrate 对辣椒素引起的继发性机械异常性疼痛有很强的增强作用。Pentoxyverine (50?mg/kg;口服) citrate 可以用作阳性对照,对任一性别的小鼠 (22-25?g) 给药7天后,使氨水诱导的咳嗽潜伏期百分比增加121.72%,抑制咳嗽频率45.45%。 Animal Model:Female wild-type weighing 25 to 30?g
Dosage:0.5, 1, 2, 4, 8, 16, 32 mg/kg
Administration:SC; 30?min before the intraplantar (i.pl.) administration of capsaicin (0.125?μg)
Result:Dose-dependently potentiated the sensitizing effect of capsaicin to the mechanical stimulus when the mice were stimulated in the paw injected with capsaicin.
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