Structure-activity relationships of histamine H-1-receptor agonists

Pertz, Heinz H. and Elz, Sigurd and Schunack, Walter (2004) Structure-activity relationships of histamine H-1-receptor agonists. MINI-REVIEWS IN MEDICINAL CHEMISTRY, 4 (9). pp. 935-940. ISSN 1389-5575

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Abstract

Significant progress in the development of potent and selective histamine H-1-receptor agonists has been achieved since 1990. Optimisation of the class of 2-phenylhistamines has furnished 2-[3(trifluoromethyl)phenyl]histamine and its N-alpha-methyl derivative. The discovery of histaprodifen (2-[2-(3,3-diphenylpropyl)-1H-imidazol-4-yl]ethanamine) and the novel lead compound suprahistaprodifen (N-alpha-2-[(1H-imidazol-4-yl)ethyl]histaprodifen) represents additional milestones in the H-1-receptor agonist field.

Item Type: Article
Uncontrolled Keywords: H-1 RECEPTOR AGONISTS; IN-VITRO EVALUATION; G-PROTEIN; 2-SUBSTITUTED HISTAMINE; HISTAPRODIFEN ANALOGS; ANESTHETIZED RAT; POTENT; DERIVATIVES; PHARMACOLOGY; LIGANDS; histaprodifen; suprahistaprodifen; H-1-receptor agonist; partial agonist; guinea-pig ileum; guinea-pig aorta; guinea-pig trachea; rat aorta
Subjects: 500 Science > 540 Chemistry & allied sciences
600 Technology > 610 Medical sciences Medicine
600 Technology > 615 Pharmacy
Divisions: Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz)
Depositing User: Petra Gürster
Date Deposited: 02 Feb 2022 06:22
Last Modified: 02 Feb 2022 06:25
URI: https://pred.uni-regensburg.de/id/eprint/37010

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