187665-65-2

中文名称 (1S)-1-[2-[4-[4-(AMINOCARBONYL)PHENYL]-1-PIPERAZINYL]ETHYL]-3,4-DIHYDRO-N-METHYL-1H-2-BENZOPYRAN-6-CARBOXAMIDE

英文名称 (1S)-1-[2-[4-[4-(AMINOCARBONYL)PHENYL]-1-PIPERAZINYL]ETHYL]-3,4-DIHYDRO-N-METHYL-1H-2-BENZOPYRAN-6-CARBOXAMIDE

CAS 187665-65-2

分子式 C24H30N4O3

分子量 422.52

MOL 文件 187665-65-2.mol

187665-65-2 结构式

基本信息物理化学性质 (1S)-1-[2-[4-[4-(AMINOCARBONYL)PHENYL]-1-PIPERAZINYL]ETHYL]-3,4-DIHYDRO-N-METHYL-1H-2-BENZOPYRAN-6-CARBOXAMIDE价格(试剂级) 常见问题列表

基本信息

中文别名

化合物 T16556

英文别名

PNU 142633
(1S)-1-[2-[4-[4-(AMINOCARBONYL)PHENYL]-1-PIPERAZINYL]ETHYL]-3,4-DIHYDRO-N-METHYL-1H-2-BENZOPYRAN-6-CARBOXAMIDE

物理化学性质

储存条件Store at +4°C

溶解度Soluble to 100 mM in DMSO

形态粉末

常见问题列表

生物活性

PNU-142633 是一种高亲和力，选择性和口服活性的 5-HT1D 激动剂，对人 5-HT1D 受体和人 5-HT1B 受体的 Ki 分别为 6 nM 和 >18 000 nM。PNU-142633 具有抗偏头痛功效。

靶点

5-HT _1D Receptor

6 nM (Ki)

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.

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.

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.