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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
7
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pubmed:dateCreated |
1988-5-10
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pubmed:abstractText |
Smooth muscle cells from the gastric antrum of the rabbit were isolated using collagenase and pronase. We examined the characteristics of muscarinic receptors that control contraction of the muscle cell: kinetics, stoichiometry and specificity of both contractile response to muscarinic agents and binding of labeled N-methyl-scopolamine. Cells contracted in the presence of muscarinic agents after a short time (30 sec) while binding of (3H)-NMS reached a plateau after 10 min exposure. Specific binding was saturable and Scatchard analysis revealed a single class of high-affinity binding sites (Kd: 0.5 nM). Oxotremorine was the most potent agonist with an ED50 of 0.6 pM; acetylcholine and carbachol were 10 times less potent. Muscarinic antagonists competed with (3H)-NMS for binding with IC50 values in the same range (nanomolar or less) than those obtained for inhibition of acetylcholine-induced contractions. Pirenzepine antagonized contractile effect of muscarinic agonists with EC50 in a micromolar range. Intracellular levels of cyclic AMP were lowered by muscarinic agonists. Monoclonal anti-muscarinic receptor antibodies M-35 displayed agonist-like activities triggering contraction and lowering cyclic AMP levels of the cells. However, although the antagonist inhibits M-35-induced contractions and cAMP decrease, M-35 had no effect on binding of the antagonist to the muscarinic receptor. These data revealed the presence of an M2-muscarinic receptor subtype involved in the contractile response of the isolated smooth muscle cell.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Acetylcholine,
http://linkedlifedata.com/resource/pubmed/chemical/Antibodies, Monoclonal,
http://linkedlifedata.com/resource/pubmed/chemical/Atropine,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclic AMP,
http://linkedlifedata.com/resource/pubmed/chemical/N-Methylscopolamine,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Muscarinic,
http://linkedlifedata.com/resource/pubmed/chemical/Scopolamine Derivatives
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
0006-2952
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
1
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pubmed:volume |
37
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1363-9
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:2833278-Acetylcholine,
pubmed-meshheading:2833278-Animals,
pubmed-meshheading:2833278-Antibodies, Monoclonal,
pubmed-meshheading:2833278-Atropine,
pubmed-meshheading:2833278-Cyclic AMP,
pubmed-meshheading:2833278-Dose-Response Relationship, Drug,
pubmed-meshheading:2833278-Muscle, Smooth,
pubmed-meshheading:2833278-Muscle Contraction,
pubmed-meshheading:2833278-N-Methylscopolamine,
pubmed-meshheading:2833278-Pyloric Antrum,
pubmed-meshheading:2833278-Rabbits,
pubmed-meshheading:2833278-Receptors, Muscarinic,
pubmed-meshheading:2833278-Scopolamine Derivatives
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pubmed:year |
1988
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pubmed:articleTitle |
Muscarinic receptors in isolated smooth muscle cells from gastric antrum.
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pubmed:affiliation |
Laboratoire de Biochimie des Membranes, CNRS ER 228, Faculté de Pharmacie, Montpelier, France.
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
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