Human Gastric Mucosa Expresses Glandular M3 Subtype of Muscarinic Receptors
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- Five subtypes of muscarinic receptors have been distinguished by pharmacological and molecular biological methods. This report characterizes the muscarinic subtype present in human gastric mucosa by radioligand binding studies. The receptor density was 27 ± 6 fmol/mg protein and the tritiated ligand N-methylscopolamine had an affinity of (Kn) 0.39 ± 0.08 nM (n = 11). The M1 receptor selective antagonist pirenzepine and the M2 receptor selective ligand AF-DX 116 had low affinities of 148 ± 32 nM (n = 13) and 4043 ± 1011 nM (n = 3) K n ,Five subtypes of muscarinic receptors have been distinguished by pharmacological and molecular biological methods. This report characterizes the muscarinic subtype present in human gastric mucosa by radioligand binding studies. The receptor density was 27 ± 6 fmol/mg protein and the tritiated ligand N-methylscopolamine had an affinity of (Kn) 0.39 ± 0.08 nM (n = 11). The M1 receptor selective antagonist pirenzepine and the M2 receptor selective ligand AF-DX 116 had low affinities of 148 ± 32 nM (n = 13) and 4043 ± 1011 nM (n = 3) K n , respectively. The glandular M3 antagonists hexahydrosiladifenidol and silahexocyclium had high affinities ofKn 78 ± 23 nM (n = 5) and 5.6 ± 1.8 nM (n = 3). The agonist carbachol interacted with a single low-affinity site and binding was insensitive to modulation by guanine nucleotides. Antagonist and agonist binding studies thus showed an affinity profile typical of M3 receptors of the glandular type.…
Autor(en): | A. Pfeiffer, C. Hanack, R. Kopp, R. Tacke, U. Moser, E. Mutschler, G. Lambrecht, M. Herawi |
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URN: | urn:nbn:de:bvb:20-opus-128286 |
Dokumentart: | Artikel / Aufsatz in einer Zeitschrift |
Institute der Universität: | Fakultät für Chemie und Pharmazie / Institut für Anorganische Chemie |
Sprache der Veröffentlichung: | Englisch |
Titel des übergeordneten Werkes / der Zeitschrift (Englisch): | Digestive Diseases and Sciences |
Erscheinungsjahr: | 1990 |
Band / Jahrgang: | 35 |
Heft / Ausgabe: | 12 |
Seitenangabe: | 1468-1472 |
Originalveröffentlichung / Quelle: | Digestive Diseases and Sciences, Val. 35, No. 12 (December 1990), pp. 1468-1472 |
Allgemeine fachliche Zuordnung (DDC-Klassifikation): | 5 Naturwissenschaften und Mathematik / 54 Chemie / 546 Anorganische Chemie |
Freie Schlagwort(e): | acid secretion; glandular M3 receptor; human gastric mucosa; muscarinic receptor subtype; stomach |
Datum der Freischaltung: | 01.03.2016 |
Lizenz (Deutsch): | Deutsches Urheberrecht |