Enantiospecific synthesis and pharmacological evaluation of a series of super-potent, conformationally restricted 5-HT2A/2C receptor agonists

JJ Chambers, DM Kurrasch-Orbaugh…

文献索引：Chambers; Kurrasch-Orbaugh; Parker; Nichols Journal of Medicinal Chemistry, 2001 , vol. 44, # 6 p. 1003 - 1010

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被引用次数: 90

摘要

The affinity of ligands for either the 5-HT2A or 5-HT2C agonist binding site was enhanced by modification of the 2, 5-oxygen substituents that are found in typical hallucinogenic amphetamines such as 4b (DOB). Restriction of the conformationally flexible 2, 5-dimethoxy substituents into fused dihydrofuran rings generally resulted in increased potency relative to the parent 2, 5-dimethoxy compounds. The pure enantiomers of these arylalkylamines ...