Structure-activity relationships of histamine H-2 receptor ligands

Dove, Stefan and Elz, Sigurd and Seifert, Roland and Buschauer, Armin (2004) Structure-activity relationships of histamine H-2 receptor ligands. MINI-REVIEWS IN MEDICINAL CHEMISTRY, 4 (9). pp. 941-954. ISSN 1389-5575, 1875-5607

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Abstract

Recent research on histamine H-2 receptor agonists was focused on quantitative structure-activity relationships and receptor models explaining the activity of imidazolylpropylguanidines. Their selectivity for guinea pig vs. human isoforms was investigated using H-2 receptor-G(salpha) fusion proteins and attributed to amino acid differences in transmembrane domains 1 and 7. New antagonists result from approaches to improve pharmacokinetic properties and to design hybrid drugs which additionally have gastroprotective or anti H. pylori activity.

Item Type: Article
Uncontrolled Keywords: HELICOBACTER-PYLORI AGENTS; AGONISTIC BINDING-SITE; GASTRIC-ACID-SECRETION; NEUROENDOCRINE CELL HYPERPLASIA; POSITIVE INOTROPIC SUBSTANCES; H-1/H-2 RECEPTOR ANTAGONISTS; PIG CEREBRAL-CORTEX; H2-RECEPTOR ANTAGONIST; H-2 RECEPTORS; GUINEA-PIG; H-2 receptor agonists; H-2 receptor antagonists; impromidine analogues; arpromidine; molecular modelling; structure-activity relationships; QSAR; site-directed mutagenesis
Subjects: 600 Technology > 610 Medical sciences Medicine
600 Technology > 615 Pharmacy
Divisions: Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz)
Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Chemistry and Pharmacy > Institute of Pharmacy > Pharmacology and Toxicology (Prof. Schlossmann, formerly Prof. Seifert)
Depositing User: Petra Gürster
Date Deposited: 02 Feb 2022 06:25
Last Modified: 02 Feb 2022 06:25
URI: https://pred.uni-regensburg.de/id/eprint/37011

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