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149247-12-1

中文名稱 149247-12-1
英文名稱 3,4-Dihydro-2-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-1(2H)-naphthalenone
CAS 149247-12-1
分子式 C23H28N2O2
分子量 364.48
MOL 文件 149247-12-1.mol
149247-12-1 結(jié)構(gòu)式 149247-12-1 結(jié)構(gòu)式

基本信息

中文別名
化合物 T10100
英文別名
QF0301B
3,4-Dihydro-2-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-1(2H)-naphthalenone
1(2H)-Naphthalenone, 3,4-dihydro-2-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜

常見(jiàn)問(wèn)題列表

生物活性
QF0301B是α1腎上腺素能受體 (α1 adrenergic receptor) 拮抗劑,也可阻斷α2腎上腺素受體,5-HT2A和組胺H1受體。
靶點(diǎn)

IC50: Adrenergic receptor

體外研究

In isolated rubbed rat aorta rings, QF0301B shows marked α1-adrenoceptor blocking activity, with a pA2 value of 9.00±0.12. QF0301B reverses and competitively antagonizes the inhibitory action produced by clonidine in electrically stimulated rat vas deferens and inhibits the force and rate of contraction in rat isolated atria (pA2=5.91±0.43), competitively antagonizes the contractile effect of 5-HT in rat aorta (pA2=6.75±0.06) and in rat stomach fundus (pA2=7.13±0.48) and the contractions induced by histamine in isolated guinea pig longitudinal ileal muscle (pA2=7.40±0.40). QF0301B shows noncompetitive low action in 5-HT3, muscarinic and nicotinic receptors, or as Ca 2+ antagonist.

體內(nèi)研究

QF0301B (0.1-0.2 mg/kg iv) can cause a pronounced and prolonged fall in mean arterial blood pressure accompanied by bradycardia. QF0301B does not significantly modify the cardiovascular effects of either 5-hydroxytryptamine (serotonin, 5-HT, 75 mg/kg iv) or the selective a2-adrenoceptor agonist B-HT 920 (0.2 mg/kg iv), but markedly inhibits the hypertensive effect of noradrenaline (5 mg/kg iv), a nonselective a-adrenergic receptor agonist.

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