Strasser, Andrea and Wittmann, Hans-Joachim and Buschauer, Armin and Schneider, Erich H. and Seifert, Roland (2013) Species-dependent activities of G-protein-coupled receptor ligands: lessons from histamine receptor orthologs. TRENDS IN PHARMACOLOGICAL SCIENCES, 34 (1). pp. 13-32. ISSN 0165-6147, 1873-3735
Full text not available from this repository. (Request a copy)Abstract
Histamine is a biogenic amine that exerts its biological effects as a neurotransmitter and local mediator via four histamine receptor (HR) subtypes (H(x)Rs) - H1R, H2R, H3R, and H4R - belonging to the superfamily of G-protein-coupled receptors (GPCRs). All four H(x)Rs exhibit pronounced differences in agonist and/or antagonist pharmacology among various species orthologs. The species differences constitute a problem for animal experiments and drug development. This problem applies to GPCRs with diverse ligands. Here, we summarize our current knowledge on HxR orthologs as a case study for species-dependent activity of GPCR ligands. We show that species-specific pharmacology also provides unique opportunities to study important aspects of GPCR pharmacology in general, including ligand-binding sites, the roles of extracellular domains in ligand binding and receptor activation, agonist-independent (constitutive) receptor activity, thermodynamics of ligand/receptor interaction, receptor-activation mechanisms, and ligand-specific receptor conformations.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | 2ND EXTRACELLULAR LOOP; H-4 RECEPTOR; GUINEA-PIG; PHARMACOLOGICAL CHARACTERIZATION; ANTAGONIST PHARMACOLOGY; BINDING THERMODYNAMICS; CONSTITUTIVE ACTIVITY; HUMAN EOSINOPHILS; PARTIAL AGONIST; N-TERMINUS; |
| Subjects: | 500 Science > 540 Chemistry & allied sciences |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) |
| Depositing User: | Petra Gürster |
| Date Deposited: | 27 May 2020 07:37 |
| Last Modified: | 27 May 2020 07:37 |
| URI: | https://pred.uni-regensburg.de/id/eprint/17483 |
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