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  • Title: Ligands of the histamine H3-receptor: new potent antagonists of the 2-thioimidazole type.
    Author: Plazzi PV, Mor M, Bordi F, Silva C, Rivara S, Caretta A, Ballabeni V, Impicciatore M, Vitali T.
    Journal: Farmaco; 1997 May; 52(5):295-302. PubMed ID: 9274000.
    Abstract:
    An overview of H3-receptor ligands is presented, with particular attention to antagonists. The protein binding of the classical H3-receptor antagonist thioperamide and its effect on in vivo distribution are discussed. A series of H3-receptor antagonists characterised by the presence of an imidazole ring, a spacer (ethylthio-, ethylamino-, propylthio- or propylamino-chain), a second heterocycle nucleus and a lipophilic group is described. Their H3-receptor antagonist potency has been measured on electrically stimulated guinea-pig intestine, and their affinity for central H3-receptor has been determined by competitive inhibition of [3H]N alpha-methylhistamine binding to rat cortex. Biphasic inhibition curves have been observed in some cases. Compounds endowed with interesting activity belong mostly to the class of 2-[[2-[4(5)-imidazolyl]ethyl]thio]imidazole, having a phenyl or a cyclohexyl group.
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