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.