| pubmed-article:3179613 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:3179613 | lifeskim:mentions | umls-concept:C0019588 | lld:lifeskim |
| pubmed-article:3179613 | lifeskim:mentions | umls-concept:C0068079 | lld:lifeskim |
| pubmed-article:3179613 | lifeskim:mentions | umls-concept:C0599278 | lld:lifeskim |
| pubmed-article:3179613 | pubmed:issue | 3 | lld:pubmed |
| pubmed-article:3179613 | pubmed:dateCreated | 1988-12-21 | lld:pubmed |
| pubmed-article:3179613 | pubmed:abstractText | 1. A series of derivatives of 4-methyldiphenhydramine have been examined as potential quaternary radioligands for the histamine H1-receptor. 2. [3H]-(+)-N-methyl-4-methyldiphenhydramine ([3H]-QMDP), 83 Ci mmol-1, was synthesized by methylation of the tertiary analogue and purified by high-voltage electrophoresis. 3. [3H]-QMDP bound to H1-receptors in a washed homogenate from guinea-pig cerebellum with an affinity constant, Ka, of 1.14 +/- 0.03 x 10(9) M-1. The proportion of non-specific binding of 0.3-0.6 nM [3H]-QMDP, defined by 0.4 microM mepyramine, was usually in the range 15-45%, depending on the method of measurement of binding. The affinity of [3H]-QMDP was similar in guinea-pig cerebellum, cerebral cortex and hippocampus, but was lower, 1.4 x 10(8) M-1, in rat cerebral cortex. 4. Evidence was obtained for the presence of a secondary, non-muscarinic, binding site for [3H]-QMDP in guinea-pig cerebellum, approximate Ka 1.5 x 10(7) M-1, accounting for circa 4% of the total binding of 1 nM [3H]-QMDP. 5. There was a very good correlation between the affinities of 15 compounds for the H1-receptor determined from inhibition of [3H]-QMDP binding and from inhibition of [3H]-mepyramine binding. 6. The potential utility of [3H]-QMDP for studies of H1-receptors in the plasma membrane of cells in culture is discussed. | lld:pubmed |
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| pubmed-article:3179613 | pubmed:language | eng | lld:pubmed |
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| pubmed-article:3179613 | pubmed:citationSubset | IM | lld:pubmed |
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| pubmed-article:3179613 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:3179613 | pubmed:month | Jul | lld:pubmed |
| pubmed-article:3179613 | pubmed:issn | 0007-1188 | lld:pubmed |
| pubmed-article:3179613 | pubmed:author | pubmed-author:YoungJ MJM | lld:pubmed |
| pubmed-article:3179613 | pubmed:author | pubmed-author:TreherneJ MJM | lld:pubmed |
| pubmed-article:3179613 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:3179613 | pubmed:volume | 94 | lld:pubmed |
| pubmed-article:3179613 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:3179613 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:3179613 | pubmed:pagination | 797-810 | lld:pubmed |
| pubmed-article:3179613 | pubmed:dateRevised | 2009-11-18 | lld:pubmed |
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| pubmed-article:3179613 | pubmed:year | 1988 | lld:pubmed |
| pubmed-article:3179613 | pubmed:articleTitle | [3H]-(+)-N-methyl-4-methyldiphenhydramine, a quaternary radioligand for the histamine H1-receptor. | lld:pubmed |
| pubmed-article:3179613 | pubmed:affiliation | Department of Pharmacology, University of Cambridge. | lld:pubmed |
| pubmed-article:3179613 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:3179613 | pubmed:publicationType | In Vitro | lld:pubmed |
| pubmed-article:3179613 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
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