Assessment of dopamine D 1 receptor affinity and efficacy of three tetracyclic conformationally-restricted analogs of SKF38393

AH Clark, JD McCorvy, VJ Watts, DE Nichols

Index: Clark, Alia H.; McCorvy, John D.; Watts, Val J.; Nichols, David E. Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 18 p. 5420 - 5431

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Citation Number: 4

Abstract

To assess the effect of conformational mobility on receptor activity, the β-phenyl substituent of dopamine D1 agonist ligands of the phenylbenzazepine class,(±)-6, 6a, 7, 8, 9, 13b- hexahydro-5H-benzo [d] naphtho [2, 1-b] azepine-11, 12-diol (8), and its oxygen and sulfur bioisosteres 9 and 10, respectively, were synthesized as conformationally-restricted analogs of SKF38393, a dopamine D1-selective partial agonist. Compounds trans-8b, 9, and 10 ...

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