1-Aminomethylbenzocycloalkanes: Conformationally Restricted Hallucinogenic Phenethylamine Analogues as Functionally Selective 5-HT2A Receptor Agonists 1

…, D Marona-Lewicka, A Gallardo-Godoy…

Index: McLean, Thomas H.; Parrish, Jason C.; Braden, Michael R.; Marona-Lewicka, Danuta; Gallardo-Godoy, Alejandra; Nichols, David E. Journal of Medicinal Chemistry, 2006 , vol. 49, # 19 p. 5794 - 5803

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Citation Number: 59

Abstract

A series of conformationally restricted analogues of the hallucinogenic phenethylamine 1 (2, 5-dimethoxy-4-bromophenethylamine, 2C-B) was synthesized to test several hypotheses concerning the bioactive conformation of phenethylamine ligands upon binding to the 5- HT2A receptor. These benzocycloalkane analogues were assayed for their receptor binding affinity and ability to activate downstream signaling pathways, and one exceptional ...