PNU-142633

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PNU-142633

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

187665-65-2

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 active5-HT_1Dreceptoragonist withK_is of 6 nM and >18 000 nM for human5-HT_1Dreceptorand human 5-HT_1Breceptor, respectively. PNU-142633 has anti-migraine efficacy^[1]^[2].

IC₅₀& Target^[1]

5-HT_1DReceptor

6 nM (Ki)

体外研究
(In Vitro)

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^[1].

体内研究
(In Vivo)

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^[1].

Animal Model:	Male Hartley guinea pigs (250-300 g) stimulated with bipolar electrode^[1]
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.

分子量

422.52

性状

Solid

Formula

C₂₄H₃₀N₄O₃

CAS 号

187665-65-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month