| pubmed-article:11090124 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:11090124 | lifeskim:mentions | umls-concept:C0035820 | lld:lifeskim |
| pubmed-article:11090124 | lifeskim:mentions | umls-concept:C0039005 | lld:lifeskim |
| pubmed-article:11090124 | lifeskim:mentions | umls-concept:C0005682 | lld:lifeskim |
| pubmed-article:11090124 | lifeskim:mentions | umls-concept:C0034826 | lld:lifeskim |
| pubmed-article:11090124 | lifeskim:mentions | umls-concept:C0086597 | lld:lifeskim |
| pubmed-article:11090124 | lifeskim:mentions | umls-concept:C1533691 | lld:lifeskim |
| pubmed-article:11090124 | lifeskim:mentions | umls-concept:C1140999 | lld:lifeskim |
| pubmed-article:11090124 | pubmed:issue | 7 | lld:pubmed |
| pubmed-article:11090124 | pubmed:dateCreated | 2000-12-20 | lld:pubmed |
| pubmed-article:11090124 | pubmed:abstractText | 1. In urinary bladder, M(2)-muscarinic receptors predominate, but it is the smaller population of M(3)-receptors which mediate detrusor contraction. This study examines the M(2) : M(3) ratio and the role of M(2)-receptors in contraction of pig urinary bladder. 2. Competition experiments with [(3)H]-QNB determined the ratio of M(2) : M(3). In functional studies, affinity values (pK(B)) for 4-DAMP, darifenacin and methoctramine were calculated. Similar experiments were performed on tissues following selective M(3)-inactivation (incubation with 40 nM 4-DAMP mustard in the presence of 1 microM methoctramine to protect M(2)-receptors), precontraction with 50 mM KCl and relaxation with isoprenaline (30 microM) or forskolin (1 microM). 3. In competition binding, displacement of [(3)H]-QNB by 4-DAMP, darifenacin and methoctramine best fitted a two-site model suggesting a predominant (70 - 80%) population of M(2)-receptors. 4. On normal detrusor in vitro, 4-DAMP and methoctramine caused surmountable antagonism of responses to carbachol with pK(B) values of 9.37+/-0.07 and 6.05+/-0.05 respectively. Darifenacin caused unsurmountable antagonism, the apparent pK(B) value being 8.61+/-0.10. 5. In tissues where the M(3)-receptors had been inactivated and cyclic AMP levels elevated, 4-DAMP and darifenacin were less potent, with apparent pK(B) values of 8.72+/-0.08 and 6.74+/-0.07. In contrast, methoctramine was more potent, the apparent pK(B) value increasing significantly to 6.86+/-0.06. 6. se data suggest that the pig bladder possesses a similar muscarinic receptor population to the human bladder and that the M(3)-receptor subtype mediates contraction of the normal detrusor muscle. However an involvement of M(2)-receptors in contraction can be observed following pharmacological manipulation of the receptor population. | lld:pubmed |
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| pubmed-article:11090124 | pubmed:language | eng | lld:pubmed |
| pubmed-article:11090124 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11090124 | pubmed:citationSubset | IM | lld:pubmed |
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| pubmed-article:11090124 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:11090124 | pubmed:month | Dec | lld:pubmed |
| pubmed-article:11090124 | pubmed:issn | 0007-1188 | lld:pubmed |
| pubmed-article:11090124 | pubmed:author | pubmed-author:YasudaKK | lld:pubmed |
| pubmed-article:11090124 | pubmed:author | pubmed-author:YamanishiTT | lld:pubmed |
| pubmed-article:11090124 | pubmed:author | pubmed-author:Chess-William... | lld:pubmed |
| pubmed-article:11090124 | pubmed:author | pubmed-author:ChappleC RCR | lld:pubmed |
| pubmed-article:11090124 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:11090124 | pubmed:volume | 131 | lld:pubmed |
| pubmed-article:11090124 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:11090124 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:11090124 | pubmed:pagination | 1482-8 | lld:pubmed |
| pubmed-article:11090124 | pubmed:dateRevised | 2009-11-18 | lld:pubmed |
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| pubmed-article:11090124 | pubmed:year | 2000 | lld:pubmed |
| pubmed-article:11090124 | pubmed:articleTitle | The role of M(2)-muscarinic receptors in mediating contraction of the pig urinary bladder in vitro. | lld:pubmed |
| pubmed-article:11090124 | pubmed:affiliation | Department of Biomedical Science, University of Sheffield, Sheffield S10 2TN. | lld:pubmed |
| pubmed-article:11090124 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:11090124 | pubmed:publicationType | In Vitro | lld:pubmed |
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