Cannon J G, Pease J P, Hamer R L, Ilhan M, Bhatnagar R K, Long J P
J Med Chem. 1984 Feb;27(2):186-9. doi: 10.1021/jm00368a014.
Series of N-alkylated derivatives of 2-amino-4,6-dihydroxyindan 3 and 6-amino-1,3-dihydroxybenzocycloheptene 2 were prepared for pharmacological testing as congeners of 2-amino-5,7-dihydroxytetralin, which elicits dopaminergic effects in a variety of assays. All of the subject compounds demonstrated a lower order of dopamine-like activity than the tetralin derivatives. Some of the subject compounds showed weak interactions with alpha 1- and beta 1-adrenoceptors, but the major determinant of activity seemed to be the nature of the N-alkyl substituent rather than ring size.
制备了2-氨基-4,6-二羟基茚满3和6-氨基-1,3-二羟基苯并环庚烯2的一系列N-烷基化衍生物,作为2-氨基-5,7-二羟基四氢萘的同系物进行药理测试,2-氨基-5,7-二羟基四氢萘在多种试验中引发多巴胺能效应。所有受试化合物的多巴胺样活性均低于四氢萘衍生物。一些受试化合物与α1和β1肾上腺素能受体表现出弱相互作用,但活性的主要决定因素似乎是N-烷基取代基的性质而非环的大小。