| pubmed-article:3754581 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:3754581 | lifeskim:mentions | umls-concept:C0034721 | lld:lifeskim |
| pubmed-article:3754581 | lifeskim:mentions | umls-concept:C0034693 | lld:lifeskim |
| pubmed-article:3754581 | lifeskim:mentions | umls-concept:C0018787 | lld:lifeskim |
| pubmed-article:3754581 | lifeskim:mentions | umls-concept:C0007776 | lld:lifeskim |
| pubmed-article:3754581 | lifeskim:mentions | umls-concept:C0022655 | lld:lifeskim |
| pubmed-article:3754581 | lifeskim:mentions | umls-concept:C0001613 | lld:lifeskim |
| pubmed-article:3754581 | lifeskim:mentions | umls-concept:C0228174 | lld:lifeskim |
| pubmed-article:3754581 | lifeskim:mentions | umls-concept:C0205145 | lld:lifeskim |
| pubmed-article:3754581 | lifeskim:mentions | umls-concept:C0031978 | lld:lifeskim |
| pubmed-article:3754581 | lifeskim:mentions | umls-concept:C0034440 | lld:lifeskim |
| pubmed-article:3754581 | lifeskim:mentions | umls-concept:C1167622 | lld:lifeskim |
| pubmed-article:3754581 | lifeskim:mentions | umls-concept:C0231491 | lld:lifeskim |
| pubmed-article:3754581 | lifeskim:mentions | umls-concept:C0851285 | lld:lifeskim |
| pubmed-article:3754581 | lifeskim:mentions | umls-concept:C0449560 | lld:lifeskim |
| pubmed-article:3754581 | lifeskim:mentions | umls-concept:C1880022 | lld:lifeskim |
| pubmed-article:3754581 | lifeskim:mentions | umls-concept:C0599668 | lld:lifeskim |
| pubmed-article:3754581 | pubmed:issue | 2 | lld:pubmed |
| pubmed-article:3754581 | pubmed:dateCreated | 1986-6-23 | lld:pubmed |
| pubmed-article:3754581 | pubmed:abstractText | Studies show [3H]PZ identified selectively a subpopulation of muscarinic binding sites compared to classical antagonists like (-)-[3H]QNB in many central and peripheral tissues. We characterized the binding and regulation of selected antagonists to high-affinity [3H]PZ (putative M1) and low-affinity PZ (putative M2) sites in rat cerebral cortex (predominantly M1) and heart (predominantly M2). Saturation isotherms of [3H]PZ and (-)-[3H]QNB were performed under various conditions. Guanyl-5'-yl-imidodiphosphate (30 microM) showed little effect on Kd (dissociation constant) or total binding capacity (total receptor density) values. Higher ionic strength buffers yielded lower affinity values for [3H]PZ and (-)-[3H]QNB. Kinetic studies confirmed high affinity Kd values seen in steady-state assays. We conducted inhibition studies of selected muscarinic antagonists including the reportedly cardioselective (putative M2) drug, AF-DX 116 (11-[(2-(diethylamino)methyl-1-piperidinyl)-acetyl]-5, 11-dihydro-6H-pyrido(2,3-b)(1,4)-benzodiazepine-6-one], the reportedly M1 selective compound, PZ, and the classical antagonist (-)QNB, using [3H]PZ and (-)-[3H]QNB-labeled cerebral cortical and cardiac homogenates. Assays were done with and without guanyl-5'-yl-imidophosphate at 25 degrees C in 10 mM Na-K-phosphate, 50 mM Na-K-phosphate and modified Krebs-phosphate buffer. Studies showed antagonists generally had higher affinity in 10 mM Na-K-phosphate buffer, were insensitive to guanyl-5'-yl imidodiphosphate and had Hill values (nH) nearly equal to one. Cardiac PZ/[3H]QNB curves were steep.(ABSTRACT TRUNCATED AT 250 WORDS) | lld:pubmed |
| pubmed-article:3754581 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
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| pubmed-article:3754581 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:3754581 | pubmed:language | eng | lld:pubmed |
| pubmed-article:3754581 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:3754581 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:3754581 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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| pubmed-article:3754581 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:3754581 | pubmed:month | May | lld:pubmed |
| pubmed-article:3754581 | pubmed:issn | 0022-3565 | lld:pubmed |
| pubmed-article:3754581 | pubmed:author | pubmed-author:YamamuraH IHI | lld:pubmed |
| pubmed-article:3754581 | pubmed:author | pubmed-author:RoeskeW RWR | lld:pubmed |
| pubmed-article:3754581 | pubmed:author | pubmed-author:WatsonMM | lld:pubmed |
| pubmed-article:3754581 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:3754581 | pubmed:volume | 237 | lld:pubmed |
| pubmed-article:3754581 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:3754581 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:3754581 | pubmed:pagination | 419-27 | lld:pubmed |
| pubmed-article:3754581 | pubmed:dateRevised | 2007-11-14 | lld:pubmed |
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| pubmed-article:3754581 | pubmed:meshHeading | pubmed-meshheading:3754581-... | lld:pubmed |
| pubmed-article:3754581 | pubmed:year | 1986 | lld:pubmed |
| pubmed-article:3754581 | pubmed:articleTitle | [3H]pirenzepine and (-)-[3H]quinuclidinyl benzilate binding to rat cerebral cortical and cardiac muscarinic cholinergic sites. II. Characterization and regulation of antagonist binding to putative muscarinic subtypes. | lld:pubmed |
| pubmed-article:3754581 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:3754581 | pubmed:publicationType | In Vitro | lld:pubmed |
| pubmed-article:3754581 | pubmed:publicationType | Research Support, U.S. Gov't, P.H.S. | lld:pubmed |
| pubmed-article:3754581 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:3754581 | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:3754581 | lld:pubmed |
