Structure-activity relationships of histamine H1-receptor agonists

  • Mini Rev Med Chem. 2004 Nov;4(9):935-40. doi: 10.2174/1389557043403198.
Heinz H Pertz  1 ,  Sigurd Elz ,  Walter Schunack
Affiliations
  • 1. Freie Universität Berlin, Institut für Pharmazie, Königin-Luise-Str. 2+4, 14195 Berlin, Germany. [email protected].
PMID: 15544554 DOI: 10.2174/1389557043403198
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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