Human Gastric Mucosa Expresses Glandular M3 Subtype of Muscarinic Receptors

Please always quote using this URN: urn:nbn:de:bvb:20-opus-128286
  • 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.show moreshow less

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Metadaten
Author: A. Pfeiffer, C. Hanack, R. Kopp, R. Tacke, U. Moser, E. Mutschler, G. Lambrecht, M. Herawi
URN:urn:nbn:de:bvb:20-opus-128286
Document Type:Journal article
Faculties:Fakultät für Chemie und Pharmazie / Institut für Anorganische Chemie
Language:English
Parent Title (English):Digestive Diseases and Sciences
Year of Completion:1990
Volume:35
Issue:12
Pagenumber:1468-1472
Source:Digestive Diseases and Sciences, Val. 35, No. 12 (December 1990), pp. 1468-1472
Dewey Decimal Classification:5 Naturwissenschaften und Mathematik / 54 Chemie / 546 Anorganische Chemie
Tag:acid secretion; glandular M3 receptor; human gastric mucosa; muscarinic receptor subtype; stomach
Release Date:2016/03/01
Licence (German):License LogoDeutsches Urheberrecht