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ChemicalBook CAS数据库列表 (1S)-1-[2-[4-[4-(AMINOCARBONYL)PHENYL]-1-PIPERAZINYL]ETHYL]-3,4-DIHYDRO-N-METHYL-1H-2-BENZOPYRAN-6-CARBOXAMIDE

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

生物活性靶点体外研究体内研究 (1S)-1-[2-[4-[4-(AMINOCARBONYL)PHENYL]-1-PIPERAZINYL]ETHYL]-3,4-DIHYDRO-N-METHYL-1H-2-BENZOPYRAN-6-CARBOXAMIDE 试剂级价格

CAS号:187665-65-2
英文名:(1S)-1-[2-[4-[4-(AMINOCARBONYL)PHENYL]-1-PIPERAZINYL]ETHYL]-3,4-DIHYDRO-N-METHYL-1H-2-BENZOPYRAN-6-CARBOXAMIDE
中文名:(1S)-1-[2-[4-[4-(AMINOCARBONYL)PHENYL]-1-PIPERAZINYL]ETHYL]-3,4-DIHYDRO-N-METHYL-1H-2-BENZOPYRAN-6-CARBOXAMIDE
CBNumber:CB82454328
分子式:C24H30N4O3
分子量:422.52
MOL File:187665-65-2.mol

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

沸点 :652.5±55.0 °C(Predicted)
密度 :1?+-.0.06 g/cm3(Predicted)
储存条件 :Store at +4°C
溶解度 :Soluble to 100 mM in DMSO
形态 :Powder
酸度系数(pKa) :15.27±0.40(Predicted)

(1S)-1-[2-[4-[4-(AMINOCARBONYL)PHENYL]-1-PIPERAZINYL]ETHYL]-3,4-DIHYDRO-N-METHYL-1H-2-BENZOPYRAN-6-CARBOXAMIDE性质、用途与生产工艺

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.