Cannon J G, O'Donnell J P, Lee T, Hoppin C R, Long J P, Ilhan M, Costall B, Naylor R J
J Med Chem. 1975 Dec;18(12):1212-6. doi: 10.1021/jm00246a008.
Secondary and tertiary amino homologs of the title compounds have been prepared, bearing an N-isopropyl group. In peripheral evaluation, certain members of the series exhibited beta-adrenergic agonist effects of lower activity than isoproterenol. N-Methyl-N-isopropyl-5,6-dihydroxytetralin exhibited marked properties consistent with its being an alpha agonist, and it is concluded that introduction of considerable bulk about the nitrogen of a catecholamine does not a priori destroy alpha-agonist effects. The compounds qualitatively paralleled the effects of dopamine in assays based upon direct intrastriatal administration in rats, although they were less potent than dopamine.
已制备出带有N - 异丙基的标题化合物的仲胺和叔胺同系物。在初步评估中,该系列中的某些成员表现出β - 肾上腺素能激动剂作用,但其活性低于异丙肾上腺素。N - 甲基 - N - 异丙基 - 5,6 - 二羟基四氢化萘表现出与其作为α激动剂相符的显著特性,并且得出结论,在儿茶酚胺的氮原子周围引入相当大的基团并不会先验地破坏α激动剂作用。在基于直接向大鼠纹状体内给药的试验中,这些化合物在性质上与多巴胺的作用相似,尽管它们的效力比多巴胺低。