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Mini-Reviews in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Structure-Activity Relationships of Histamine H1-Receptor Agonists

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

Volume 4, Issue 9, 2004

Page: [935 - 940] Pages: 6

DOI: 10.2174/1389557043403198

Price: $65

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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.

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


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