Structure-Activity Relationships of Histamine H1-Receptor Agonists

Title: Structure-Activity Relationships of Histamine H1-Receptor Agonists

Volume: 4 Issue: 9

Author(s): Heinz H. Pertz, Sigurd Elz and Walter Schunack

Affiliation:

Keywords: histaprodifen, suprahistaprodifen, h1-receptor agonist, partial agonist, guinea-pig ileum, guinea-pig aorta, guineapig trachea, rat aorta

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 Nα-methyl derivative. The discovery of histaprodifen (2-[2-(3,3- diphenylpropyl)-1H-imidazol-4-yl]ethanamine) and the novel lead compound suprahistaprodifen (Nα-2-[(1Himidazol- 4-yl)ethyl]histaprodifen) represents additional milestones in the H1-receptor agonist field.

Cite this article as:

Pertz H. Heinz, Elz Sigurd and Schunack Walter, Structure-Activity Relationships of Histamine H1-Receptor Agonists, Mini-Reviews in Medicinal Chemistry 2004; 4 (9) . https://dx.doi.org/10.2174/1389557043403198