与拉贝洛尔和甲磺酸美多心安相关的抗高血压氨基四氢萘类药物。
Antihypertensive aminotetralins related to labetalol and medroxalol.
作者信息
Clark R D, Caroon J M, Repke D B, Strosberg A M, Whiting R L, Brown C M
出版信息
J Pharm Sci. 1986 Jan;75(1):80-2. doi: 10.1002/jps.2600750119.
A series of compounds was prepared in which the 1-methyl-3-phenylpropylamino moieties of the antihypertensive agents labetalol and medroxalol were replaced by 2-aminotetralins. Compounds containing a 6-methoxy and 6,7-methylenedioxy group in the aminotetralin were at least as active as labetalol in lowering the blood pressure of the spontaneously hypertensive rat (SHR). As determined by ligand binding, these compounds were comparable to labetalol as alpha 1-antagonists but were substantially weaker beta 1-antagonists.
制备了一系列化合物，其中抗高血压药拉贝洛尔和甲磺酸美多心安的1-甲基-3-苯基丙基氨基部分被2-氨基四氢萘取代。在氨基四氢萘中含有6-甲氧基和6,7-亚甲二氧基的化合物在降低自发性高血压大鼠（SHR）血压方面至少与拉贝洛尔活性相当。通过配体结合测定，这些化合物作为α1拮抗剂与拉贝洛尔相当，但作为β1拮抗剂则明显较弱。
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