熔点 | 115.0°C-119.0°C |
溶解性 | Soluble in DMSO (>25 mg/ml), ethanol (10 mg/ml), methanol (33.8 mg/ml), phosphate buffer (pH 4) (0.43 mg/ml) at 37 °C, water (partly miscible), chloroform, methylene chloride, and ethyl ether (slightly soluble). Insoluble in isopropanol. |
应用 | An α1- and β-adrenergic receptor antagonist. |
产品介绍 | Carvedilol是一种非选择性β/α-1受体抑制剂,用于治疗充血性心力衰竭和高血压。 |
生化机理 | Carvedilol is a AR (α1 and β-adrenergic receptor) antagonist with antioxidant properties. Studies show that the receptors α1D-AR and α1B-AR have a greater affinity for Carvedilol in comparison to the receptor β1-AR subtype. Carvedilol has been observed to block the oscillatory intracellular calcium changes induced by α1D-AR and α1B-AR, and shown to have a higher oxidative effect than Atenolol. The S(-) enantiomer of Carvedilol acts as a β-blocker, and the R(+) and S (-) enantionmers both block the α1. Carvedilol is an inhibitor of α1B-AR, β1-AR, β2-AR and α1D-AR. |
别名 | 卡维地洛;1-(9H-咔唑-4-氧基)-3-[2-(2-甲氧基苯氧基)乙基氨基]-2-丙醇1-?(9H-?Carbazol-?4-?yloxy)?-?3-?[[2-?(2-?methoxyphenoxy)?ethyl]?amino]?-?2-?propanol;BM-14190;BM 14190;BM14190 |