Aminimides as potential CNS-acting agents. III. Design, synthesis, and receptor binding of aminimide analogues of dopamine, serotonin, morphine, and nicotine

Benny Capuano, Ian Travers Crosby, Edward John Lloyd, Juliette E Neve, David Taylor

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A series of aminimide derivatives of centrally acting agents, namely dopamine, serotonin, morphine and nicotine, were designed on the basis of the physicochemical properties of the aminimide functional group and synthesized to investigate their central nervous system (CNS) receptor affinity. The target compounds were readily prepared from an appropriate tertiary amine by N-acylation of a hydrazinium salt intermediate using acetic anhydride or acetyl chloride. The aminimides were tested for in vitro affinity at the dopaminergic D-4, serotonergic 5-HT2A, opiate (mu, kappa, and non-selective) and nicotinic acetylcholine receptors and were found to possess mixed affinities for the aforementioned receptor systems.
Original languageEnglish
Pages (from-to)422 - 431
Number of pages10
JournalAustralian Journal of Chemistry
Issue number6
Publication statusPublished - 2008

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