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  • Title: In vitro characterization of potency, affinity and selectivity of H3-antagonists: from thioperamide to thioperamide unrelated imidazole derivatives.
    Author: Barocelli E, Ballabeni V, Caretta A, Bertoni S, Bordi F, Rivara S, Silva C, Mor M, Impicciatore M.
    Journal: Farmaco; 1997; 52(6-7):463-9. PubMed ID: 9372599.
    Abstract:
    This paper summarizes the findings obtained for three different series of original compounds designed as potential H3-antagonists starting from thioperamide structure. The compounds were tested in functional and binding assays to estimate their potency, affinity and selectivity for histamine H3 receptors. Among them, many non-thiourea/isothiourea derivatives acted as selective H3 competitive antagonists and, particularly, 4(5)-[2-[4(5)-cyclohexylimidazol-2-ylthio]ethyl] imidazole (dIII) proved to be the most potent H3 blocker vs (R)-alpha-methylhistamine in electrically-stimulated ileum. This imidazole derivative, devoid of thiourea dependent toxic effects, with high affinity displaced biphasically [3H]-N alpha-methylhistamine bound to rat brain H3 sites. Thus, such compound could be proposed as the prototype molecule for the development of new non-thiourea/isothiourea H3-antagonists and as experimental tool to explore the intriguing question of H3 receptor heterogeneity.
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