187665-65-2
中文名稱
(1S)-1-[2-[4-[4-(AMINOCARBONYL)PHENYL]-1-PIPERAZINYL]ETHYL]-3,4-DIHYDRO-N-METHYL-1H-2-BENZOPYRAN-6-CARBOXAMIDE
英文名稱
(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 結(jié)構(gòu)式
基本信息
中文別名
化合物 T16556 英文別名
PNU 142633(1S)-1-[2-[4-[4-(AMINOCARBONYL)PHENYL]-1-PIPERAZINYL]ETHYL]-3,4-DIHYDRO-N-METHYL-1H-2-BENZOPYRAN-6-CARBOXAMIDE
物理化學(xué)性質(zhì)
沸點(diǎn)652.5±55.0 °C(Predicted)
密度1?+-.0.06 g/cm3(Predicted)
儲(chǔ)存條件Store at +4°C
溶解度Soluble to 100 mM in DMSO
酸度系數(shù)(pKa)15.27±0.40(Predicted)
形態(tài)粉末
顏色White to off-white
常見問題列表
生物活性
PNU-142633 是一種高親和力，選擇性和口服活性的 5-HT1D 激動(dòng)劑，對(duì)人 5-HT1D 受體和人 5-HT1B 受體的 Ki 分別為 6 nM 和 >18 000 nM。PNU-142633 具有抗偏頭痛功效。靶點(diǎn)
|
5-HT 1D Receptor 6 nM (Ki) |
體外研究
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.
體內(nèi)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. |