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Updated: Aug 20, 2026

Quantifying Agonist Activity at G Protein-coupled Receptors
Published on: December 26, 2011
Structure-activity relationships of histamine H1-receptor agonists
Heinz H Pertz1, Sigurd Elz, Walter Schunack
1Freie Universität Berlin, Institut für Pharmazie, Königin-Luise-Str. 2+4, 14195 Berlin, Germany. hpertz@zedat.fu-berlin.de.
Abstract:
Significant progress in the development of potent and selective histamine H1-receptor agonists has been achieved since 1990. Optimisation of the class of 2-phenylhistamines has furnished 2-[3-(trifluoromethyl)phenyl]histamine and its Nalpha-methyl derivative. The discovery of histaprodifen (2-[2-(3,3-diphenylpropyl)-1H-imidazol-4-yl]ethanamine) and the novel lead compound suprahistaprodifen (Nalpha-2-[(1H-imidazol-4-yl)ethyl]histaprodifen) represents additional milestones in the H1-receptor agonist field.
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