PNU-142633|cas:187665-65-2|西域试剂

PNU-142633,98.0%

产品编号：Bellancom-103131| CAS NO：187665-65-2| 分子式：C₂₄H₃₀N₄O₃| 分子量：422.52

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-103131		￥11750.00	杭州北京（现货）

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PNU-142633

产品介绍

PNU-142633 是一种高亲和力，选择性和口服活性的 5-HT_1D 激动剂，对人 5-HT_1D 受体和人 5-HT_1B 受体的 K_i 分别为 6 nM 和 >18 000 nM。PNU-142633 具有抗偏头痛功效。

生物活性

PNU-142633 is a high affinity, selective and orally active 5-HT_1D receptor agonist with K_is of 6 nM and > 18 000 nM for human 5-HT_1D receptor and human 5-HT_1B receptor, respectively. PNU-142633 has anti-migraine efficacy.

体外研究

The intrinsic activity of PNU-142633 at the human 5-HT1D receptor is determined to be 70% that of 5-HT in a cytosensor cell-based assay compared with 84% for that of Sumatriptan.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

PNU-142633 (0.03-1 mg/kg; intravenous injection; male Hartley guinea pigs) treatment blocks neurogenic plasma protein extravasation. And PNU-142633 fails to alter resistance in these vascular beds.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Hartley guinea pigs (250-300 g) stimulated with bipolar electrode
Dosage:	0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg
Administration:	Intravenous injection
Result:	Significantly reduced extravasation at the 0.1 and 0.3 mg/kg doses, but was without effect at the 0.03 and 1.0 mg/kg doses.

体内研究

PNU-142633 (0.03-1 mg/kg; intravenous injection; male Hartley guinea pigs) treatment blocks neurogenic plasma protein extravasation. And PNU-142633 fails to alter resistance in these vascular beds.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Hartley guinea pigs (250-300 g) stimulated with bipolar electrode
Dosage:	0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg
Administration:	Intravenous injection
Result:	Significantly reduced extravasation at the 0.1 and 0.3 mg/kg doses, but was without effect at the 0.03 and 1.0 mg/kg doses.