Effects of barbiturates on A1 adenosine receptors of rat brain
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- Barbiturates inhibit binding of radioligands to A 1(Ri) adenosine receptors of rat brain membranes. This inhibition is dose-dependent and stereospecific and occurs in the range of pharmacologically active concentrations. The displacement of radiolabelled A1antagonists by barbiturates is not modified by GTP, indicating that barbiturates might act as antagonists at this receptor. This action of barbiturates does not seem to be related to the binding of barbiturates to plasma membranes, as the latter process has different characteristics.Barbiturates inhibit binding of radioligands to A 1(Ri) adenosine receptors of rat brain membranes. This inhibition is dose-dependent and stereospecific and occurs in the range of pharmacologically active concentrations. The displacement of radiolabelled A1antagonists by barbiturates is not modified by GTP, indicating that barbiturates might act as antagonists at this receptor. This action of barbiturates does not seem to be related to the binding of barbiturates to plasma membranes, as the latter process has different characteristics. Barbiturates also inhibit the binding of radioligands to solubilized A1receptors, and saturation and kinetic experiments suggest that this is due to a competitive antagonism. These results indicate that barbiturates interact with the recognition site of the A1adenosine receptor.…
Autor(en): | Martin J. Lohse, Karl-Norbert Klotz, Ulrich Schwabe |
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URN: | urn:nbn:de:bvb:20-opus-70100 |
Dokumentart: | Aufsatz in einem Sammelband / Buchkapitel |
Institute der Universität: | Medizinische Fakultät / Institut für Pharmakologie und Toxikologie |
Sprache der Veröffentlichung: | Englisch |
Erscheinungsjahr: | 1985 |
Originalveröffentlichung / Quelle: | In: Adenosine: receptors and modulation of cell funtion / V. Stefanovic ... eds. - Oxford [u.a.]: IRL Pr., 1985, S.221-231. - ISBN: 0-947946-49-7 |
Allgemeine fachliche Zuordnung (DDC-Klassifikation): | 6 Technik, Medizin, angewandte Wissenschaften / 61 Medizin und Gesundheit / 610 Medizin und Gesundheit |
Normierte Schlagworte (GND): | Barbiturat; Adenosinrezeptor; Ratte |
Datum der Freischaltung: | 19.05.2014 |
Lizenz (Deutsch): | Deutsches Urheberrecht |