| 生物活性: |
靶点:Adrenergic Receptor 通路:Endocrinology & Hormones;GPCR & G Protein;Neuronal Signaling 背景说明:是一种非选择性α-肾上腺素能拮抗剂。 生物活性:Phentolamine Mesylate 是一种非选择性的 α1 和 α2 肾上腺素能受体阻滞剂,可扩张血管以降低外周血管阻力。[1-3] In Vitro:甲磺酸酚妥拉明对氯尼定的pKB 值为8.07 [2]。甲磺酸酚妥拉明酚妥拉明可抑制 HDMECs 和 HBMECs 的增殖、迁移和微管生成[3]。 In Vivo:静脉或口服甲磺酸酚妥拉明可抑制室性早搏和室上性早搏[1]。甲磺酸酚妥拉明(1 毫克/千克,静脉注射)可使肾动脉血管扩张,而其他血管床则无变化。[4] 数据来源文献:[1]. Gould L,et al. Phentolamine. Am Heart J. 1976 Sep;92(3):397-402. [2]. Liu L,et al. Evidence for functional alpha 2D-adrenoceptors in the rat intestine. Br J Pharmacol. 1996 Mar;117(5):787-92. [3]. Pan L,et al. Phentolamine inhibits angiogenesis in vitro: Suppression of proliferation migration and differentiation of human endothelial cells. Clin Hemorheol Microcirc. 2017;65(1):31-41. [4]. Fioretti AC,et al. Renal and femoral venous blood flows are regulated by different mechanisms dependent on α-adrenergic receptor subtypes and nitric oxide in anesthetized rats. Vascul Pharmacol. 2017 Dec;99:53-64.
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| 其它标识: |
EC:EINECS 200-604-6 MDL:MFCD00134201 SMILES:CC1=CC=C(C=C1)N(CC2=NCCN2)C3=CC(=CC=C3)O.CS(=O)(=O)O InChIKey:OGIYDFVHFQEFKQ-UHFFFAOYSA-N InChI:InChI=1S/C17H19N3O.CH4O3S/c1-13-5-7-14(8-6-13)20(12-17-18-9-10-19-17)15-3-2-4-16(21)11-15;1-5(2,3)4/h2-8,11,21H,9-10,12H2,1H3,(H,18,19);1H3,(H,2,3,4) PubChem CID:91430
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| 基本信息: |
CAS:65-28-1 中文名称:甲磺酸酚妥拉明 英文名称:Phentolamine Mesylate 别名:Phentolamine methanesulfonate 分子式:C18H23N3O4S 分子量:377.46 规格:100mg ; 50mg 溶解性:Soluble in Water/DMSO(Need ultrasonic) 纯度:≥98% 外观(性状):White to off-white Solid 储存条件:Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
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| 靶点: |
Adrenergic Receptor |