Carbachol stimulates inositol phosphate formation in rat thalamus slices through muscarinic M3-receptor activation. 1996

M T de la Vega, and A Nunez, and J A Montano
Departmento de Fisiología, Biofisica y Neurociencias, Centro de Investigación y de Estudios Avanzados, México, D.F, México.

In cross-chopped slices from rat thalamus and in the presence of 10 mM LiC1, the cholinergic agonist carbachol stimulated the accumulation of total [3H]inositol phosphates ([3H]IP2 = [3H]IP1 + [3H]IP2 + [3H]IP3). Best-fit values for the concentration-response curve for carbachol after 60 min incubation yielded an EC50 of 44 +/- 6 microM, maximum effect of 199 +/- 6% of basal accumulation and Hill coefficient (nH) of 1.1 +/- 0.1. Carbachol-induced [3H]IPs accumulation was inhibited by 4-diphenylacetoxy-N-methylpiperidine methiodide (4-DAMP; pKi 9.1) and the p-fluoro analogue of hexahydro-sila-difenidol (pF-HHSiD; pKi 8.1). Concentration-response curves for carbachol were shifted to the right in a parallel fashion by pirenzepine (100, 300 and 100 nM). A Schild plot of the data was linear (slope 0.95 +/- 0.04) and yielded a log KD for pirenzepine of -6.8 +/- 0.1. Taken together, these results suggest that carbachol-induced inositol phosphate accumulation in rat thalamus is mediated by muscarinic M3-receptors.

UI MeSH Term Description Entries
D007295 Inositol Phosphates Phosphoric acid esters of inositol. They include mono- and polyphosphoric acid esters, with the exception of inositol hexaphosphate which is PHYTIC ACID. Inositol Phosphate,Phosphate, Inositol,Phosphates, Inositol
D008297 Male Males
D009924 Organ Culture Techniques A technique for maintenance or growth of animal organs in vitro. It refers to three-dimensional cultures of undisaggregated tissue retaining some or all of the histological features of the tissue in vivo. (Freshney, Culture of Animal Cells, 3d ed, p1) Organ Culture,Culture Technique, Organ,Culture Techniques, Organ,Organ Culture Technique,Organ Cultures
D010880 Piperidines A family of hexahydropyridines.
D010890 Pirenzepine An antimuscarinic agent that inhibits gastric secretion at lower doses than are required to affect gastrointestinal motility, salivary, central nervous system, cardiovascular, ocular, and urinary function. It promotes the healing of duodenal ulcers and due to its cytoprotective action is beneficial in the prevention of duodenal ulcer recurrence. It also potentiates the effect of other antiulcer agents such as CIMETIDINE and RANITIDINE. It is generally well tolerated by patients. Gastrotsepin,Gastrozepin,L-S 519,LS-519,Piren-Basan,Pirenzepin,Pirenzepin Von Ct,Pirenzepin-Ratiopharm,Pirenzepine Dihydrochloride,Pyrenzepine,Ulcoprotect,Ulgescum,Dihydrochloride, Pirenzepine,LS 519,LS519,Piren Basan,Pirenzepin Ratiopharm,Von Ct, Pirenzepin
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
D002217 Carbachol A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS. Carbamylcholine,Carbacholine,Carbamann,Carbamoylcholine,Carbastat,Carbocholine,Carboptic,Doryl,Isopto Carbachol,Jestryl,Miostat,Carbachol, Isopto
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001667 Binding, Competitive The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements. Competitive Binding

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