Structure-activity relationships for the binding of arylpiperazines and arylbiguanides at 5-HT3 serotonin receptors

M Dukat, AA Abdel-Rahman, AM Ismaiel…

Index: Dukat, Malgorzata; Abdel-Rahman, Ashraf A.; Ismaiel, Abd M.; Ingher, Stacy; Teitler, Milt; Gyermek, Laszlo; Glennon, Richard A. Journal of Medicinal Chemistry, 1996 , vol. 39, # 20 p. 4017 - 4026

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Citation Number: 64

Abstract

Arylpiperazines are nonselective agents that bind at 5-HT3 serotonin receptors with moderate to high affinity, whereas 1-phenylbiguanide is a low-affinity but more selective 5- HT3 agonist. In an attempt to enhance the affinity of the latter agent, and working with the assumption that similarities might exist between the binding of the two types of agents, we formulated structure-activity relationships for the binding of the arylpiperazines and then ...