Atwal K S, O'Reilly B C, Ruby E P, Turk C F, Aberg G, Asaad M M, Bergey J L, Moreland S, Powell J R
J Med Chem. 1987 Apr;30(4):627-35. doi: 10.1021/jm00387a008.
Substituted 1,2,3,4-tetrahydroaminonaphthols were found to be calcium channel blockers with antihypertensive properties. These compounds also possessed adrenergic beta-receptor blocking activity. From the structure-activity studies, no clear correlation emerged between the in vitro calcium channel blocking activity and the acute anti-hypertensive activity in cannulated spontaneously hypertensive rats. Extensive pharmacological testing of selected compounds indicated that aminonaphthols are antihypertensive agents with many pharmacological properties. The relative contribution of various pharmacological actions toward the observed antihypertensive activity is unclear. Since the clinically useful calcium channel blocker verapamil is structurally related to these compounds, one of the aminonaphthols, trans-3-[(3,3-diphenylpropyl)amino]-1,2,3,4-tetrahydro-6,7 -dimethoxy-2-naphthalenol (12), was compared with verapamil for calcium channel blocking activity, adrenergic blocking activity, and catecholamine-depleting activity. Both compounds were found to be equipotent in these test systems.
已发现取代的1,2,3,4-四氢氨基萘酚是具有抗高血压特性的钙通道阻滞剂。这些化合物还具有肾上腺素能β受体阻断活性。从构效关系研究来看，在体外钙通道阻断活性与插管自发性高血压大鼠的急性抗高血压活性之间未出现明确的相关性。对选定化合物进行的广泛药理学测试表明，氨基萘酚是具有多种药理特性的抗高血压药物。各种药理作用对所观察到的抗高血压活性的相对贡献尚不清楚。由于临床上有用的钙通道阻滞剂维拉帕米在结构上与这些化合物相关，因此将其中一种氨基萘酚反式-3-[(3,3-二苯基丙基)氨基]-1,2,3,4-四氢-6,7-二甲氧基-2-萘酚（12）与维拉帕米在钙通道阻断活性、肾上腺素能阻断活性和儿茶酚胺耗竭活性方面进行了比较。发现这两种化合物在这些测试系统中效力相当。
