Design of potent non-thiourea H3-receptor histamine antagonists

…, M Garbarg, X Ligneau, JC Schwartz

Index: Ganellin; Hosseini; Khalaf; Tertiuk; Arrang; Garbarg; Ligneau; Schwartz Journal of Medicinal Chemistry, 1995 , vol. 38, # 17 p. 3342 - 3350

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Citation Number: 39

Abstract

The histamine Ha-receptor was first characterized pharmacologically and reported'in 1983. It was shown to be located presynaptically on histaminergic neurones in the central nervous system (CNS), where it functions as an autoreceptor to modulate histamine release. The H3- receptor also modulates the synthesis of histamine from L-histidine. 2 Thus, activation of the Hs-receptor by histamine leads to a decrease in the concentration of the neurotransmitter ...