Inhibitors of neuronal monoamine uptake. 2. Selective inhibition of 5-hydroxytryptamine uptake by. alpha.-amino acid esters of phenethyl alcohols

UH Lindberg, SO Thorberg, S Bengtsson…

Index: Lindberg; Thorberg; Bengtsson; Renyi; Ross; Ogren Journal of Medicinal Chemistry, 1978 , vol. 21, # 5 p. 448 - 456

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Citation Number: 76

Abstract

A series of a-amino acid esters of substituted phenethyl alcohols was prepared and tested as inhibitors of the neuronal reuptake of noradrenaline and 5-hydroxytryptamine. Some of the compounds are potent and very selective in blocking the 5-hydroxytryptamine uptake, as evidenced by biochemical data and behavioral tests. The most promising agent, alaproclate [2-(4-chlorophenyl)-l, l-dimethylethyl2-aminopropanoate hydrochloride (1, IV)], was ...