Synthesis, absolute configuration, stereoselectivity, and receptor selectivity of (. alpha. R,. beta. S)-. alpha.,. beta.-dimethylhistamine. A novel highly potent histamine …

R Lipp, JM Arrang, M Garbarg, P Luger…

Index: Lipp; Arrang; Garbarg; Luger; Schwartz; Schunack Journal of Medicinal Chemistry, 1992 , vol. 35, # 23 p. 4434 - 4441

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Citation Number: 36

Abstract

Depending on the selected synthetic pathway, structural variations of the neurotransmitter histamine led to mixtures of a,@-dimethylhistamines as well as to the corresponding pure optical isomers. One of these isomers, namely (crR, flS)-a, fl-dimethylhistamine, proved to be a highly potent H3 receptor agonist with exceptional receptor selectivity. The absolute configuration of the compound was determined by X-ray structure analysis of ita ...