149247-12-1

149247-12-1

中文名称149247-12-1
中文同义词化合物 T10100
英文名称3,4-Dihydro-2-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-1(2H)-naphthalenone
英文同义词3,4-Dihydro-2-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-1(2H)-naphthalenone;QF0301B;1(2H)-Naphthalenone, 3,4-dihydro-2-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-;QF0301B,QF-0301B
CAS号149247-12-1
分子式C23H28N2O2
分子量364.48062
EINECS号
相关类别
Mol文件149247-12-1.mol
结构式149247-12-1 结构式

149247-12-1 性质

储存条件Store at -20°C
溶解度溶于二甲基亚砜

149247-12-1 用途与合成方法

QF0301B是α1肾上腺素能受体 (α1 adrenergic receptor) 拮抗剂,也可阻断α2肾上腺素受体,5-HT2A和组胺H1受体。

IC50: Adrenergic receptor

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.

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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149247-12-1 上下游产品信息

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