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Updated: Aug 17, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
General construction pattern of histamine H3-receptor antagonists: change of a paradigm
H Stark1, X Ligneau, J M Arrang
1Institut für Pharmazie I, Freie Universität Berlin, Germany. stark@schunet.pharmazie.fu-berlin.de
Abstract:
Novel omega-phenyl substituted and unsubstituted alkyl and alkenyl imidazole derivatives were prepared and tested for their antagonist activity in vitro and in vivo at histamine H3-receptors. Some compounds showed high in vitro and in vivo H3-receptor activity despite their structure bearing no polar moiety in the centre of the molecule which is a common structural feature of all other antagonists known. Quite probably there are further in vivo effects for some compounds resulting from other receptor interactions.
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