Muscarinic cholinergic receptors in human gastric mucosa. 1984

T Tokunaga, and R Nishimura, and M Akagi

Muscarinic cholinergic receptor sites in human gastric mucosa were analyzed directly by using radioligand binding techniques with the specific muscarinic antagonist 3H-quinuclidinyl benzilate (QNB) as ligand. Specific binding of 3H-QNB to membrane preparations from human gastric mucosa was saturable, of high affinity (Kd = 4.17 +/- 1.94 nM, Bmax = 0.37 +/- 0.04 pmol/mg protein) and selectively inhibited by muscarinic antagonists (atropine, scopolamine) and agonists (acetylcholine, pilocarpine). These findings provide direct evidence for the existence of muscarinic cholinergic receptors in human gastric mucosa. The specific 3H-QNB binding to its receptor was blocked by atropine but not by histamine, cimetidine, pentagastrin, or synthetic human gastrin. The muscarine and histamine H2-receptor, or muscarine and gastrin receptor, probably do not share the same locus.

UI MeSH Term Description Entries
D010418 Pentagastrin A synthetic pentapeptide that has effects like gastrin when given parenterally. It stimulates the secretion of gastric acid, pepsin, and intrinsic factor, and has been used as a diagnostic aid. Acignost,Gastrin Pentapeptide,Peptavlon,Pentapeptide, Gastrin
D010862 Pilocarpine A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma. Isopilocarpine,Isoptocarpine,Ocusert,Pilocarpine Hydrochloride,Pilocarpine Mononitrate, (3S-cis)-Isomer,Pilocarpine Nitrate,Pilocarpine, Monohydrochloride, (3S-cis)-Isomer,Salagen,Hydrochloride, Pilocarpine,Nitrate, Pilocarpine
D011813 Quinuclidinyl Benzilate A high-affinity muscarinic antagonist commonly used as a tool in animal and tissue studies. Benzilate, Quinuclidinyl
D011869 Radioligand Assay Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders). Protein-Binding Radioassay,Radioreceptor Assay,Assay, Radioligand,Assay, Radioreceptor,Assays, Radioligand,Assays, Radioreceptor,Protein Binding Radioassay,Protein-Binding Radioassays,Radioassay, Protein-Binding,Radioassays, Protein-Binding,Radioligand Assays,Radioreceptor Assays
D011976 Receptors, Muscarinic One of the two major classes of cholinergic receptors. Muscarinic receptors were originally defined by their preference for MUSCARINE over NICOTINE. There are several subtypes (usually M1, M2, M3....) that are characterized by their cellular actions, pharmacology, and molecular biology. Muscarinic Acetylcholine Receptors,Muscarinic Receptors,Muscarinic Acetylcholine Receptor,Muscarinic Receptor,Acetylcholine Receptor, Muscarinic,Acetylcholine Receptors, Muscarinic,Receptor, Muscarinic,Receptor, Muscarinic Acetylcholine,Receptors, Muscarinic Acetylcholine
D002927 Cimetidine A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output. Altramet,Biomet,Biomet400,Cimetidine HCl,Cimetidine Hydrochloride,Eureceptor,Histodil,N-Cyano-N'-methyl-N''-(2-(((5-methyl-1H-imidazol-4-yl)methyl)thio)ethyl)guanidine,SK&F-92334,SKF-92334,Tagamet,HCl, Cimetidine,Hydrochloride, Cimetidine,SK&F 92334,SK&F92334,SKF 92334,SKF92334
D005744 Gastric Acid Hydrochloric acid present in GASTRIC JUICE. Hydrochloric Acid, Gastric,Acids, Gastric,Acids, Gastric Hydrochloric,Gastric Acids,Gastric Hydrochloric Acid,Gastric Hydrochloric Acids,Hydrochloric Acids, Gastric
D005753 Gastric Mucosa Lining of the STOMACH, consisting of an inner EPITHELIUM, a middle LAMINA PROPRIA, and an outer MUSCULARIS MUCOSAE. The surface cells produce MUCUS that protects the stomach from attack by digestive acid and enzymes. When the epithelium invaginates into the LAMINA PROPRIA at various region of the stomach (CARDIA; GASTRIC FUNDUS; and PYLORUS), different tubular gastric glands are formed. These glands consist of cells that secrete mucus, enzymes, HYDROCHLORIC ACID, or hormones. Cardiac Glands,Gastric Glands,Pyloric Glands,Cardiac Gland,Gastric Gland,Gastric Mucosas,Gland, Cardiac,Gland, Gastric,Gland, Pyloric,Glands, Cardiac,Glands, Gastric,Glands, Pyloric,Mucosa, Gastric,Mucosas, Gastric,Pyloric Gland
D005755 Gastrins A family of gastrointestinal peptide hormones that excite the secretion of GASTRIC JUICE. They may also occur in the central nervous system where they are presumed to be neurotransmitters. Gastrin
D006632 Histamine An amine derived by enzymatic decarboxylation of HISTIDINE. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter. Ceplene,Histamine Dihydrochloride,Histamine Hydrochloride,Peremin

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