| pubmed-article:6132001 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:6132001 | lifeskim:mentions | umls-concept:C0022646 | lld:lifeskim |
| pubmed-article:6132001 | lifeskim:mentions | umls-concept:C1882598 | lld:lifeskim |
| pubmed-article:6132001 | lifeskim:mentions | umls-concept:C0005456 | lld:lifeskim |
| pubmed-article:6132001 | lifeskim:mentions | umls-concept:C0205369 | lld:lifeskim |
| pubmed-article:6132001 | lifeskim:mentions | umls-concept:C0140805 | lld:lifeskim |
| pubmed-article:6132001 | pubmed:issue | 1 | lld:pubmed |
| pubmed-article:6132001 | pubmed:dateCreated | 1983-5-27 | lld:pubmed |
| pubmed-article:6132001 | pubmed:abstractText | The binding of the novel ligand [3H]Ro 5-4864 to membrane preparations of rat kidney and brain was studied. [3H]Ro 5-4864 binds with high affinity (Kd = 0.6 nM) to a single saturable population of benzodiazepine recognition sites on renal membranes. Binding is rapidly reversible and, based on its pharmacological spectrum, takes place at the peripheral-type, Ro 5-4864-sensitive receptor. Specific high-affinity (Kd = 1.1 nM) [3H] Ro 5-4864 binding to the peripheral-type benzodiazepine binding site can also be demonstrated using rat brain membranes. [3H] Ro 5-4864 lacks stereospecificity with regard to chiral activity in position 3. A comparison of benzodiazepine inhibitory potency and structural features reveals that whereas a 4'-substitution assures specificity for the peripheral-type receptor, an N-methyl moiety is essential for optimal activity. [3H]Ro 5-4864 binding to brain membranes is temperature sensitive and is not modulated by barbiturates, convulsants, gamma-aminobutyric acid and chloride anions. The pyrazolopyridine derivative tracazolate inhibits [3H] Ro 5-4864 binding. The regional and subcellular distribution of binding is distinctly different from that previously demonstrated for [3H]benzodiazepine binding in the brain. The olfactory bulb shows the highest binding density, whereas the cerebral cortical, striatal and hippocampal areas are lowest among those areas studied. In the brain, [3H]Ro 5-4864 binding was found to sediment with the nuclear fraction. In conclusion, the present study shows that [3H]Ro 5-4864 is a selective ligand of the peripheral-type benzodiazepine binding site that can unequivocally be demonstrated in the kidney as well as the brain. The physiological significance of these findings, however, remain to be established. | lld:pubmed |
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| pubmed-article:6132001 | pubmed:language | eng | lld:pubmed |
| pubmed-article:6132001 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:6132001 | pubmed:citationSubset | IM | lld:pubmed |
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| pubmed-article:6132001 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:6132001 | pubmed:month | Apr | lld:pubmed |
| pubmed-article:6132001 | pubmed:issn | 0022-3565 | lld:pubmed |
| pubmed-article:6132001 | pubmed:author | pubmed-author:YamamuraH IHI | lld:pubmed |
| pubmed-article:6132001 | pubmed:author | pubmed-author:HorstW DWD | lld:pubmed |
| pubmed-article:6132001 | pubmed:author | pubmed-author:SchoemakerHH | lld:pubmed |
| pubmed-article:6132001 | pubmed:author | pubmed-author:BolesR GRG | lld:pubmed |
| pubmed-article:6132001 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:6132001 | pubmed:volume | 225 | lld:pubmed |
| pubmed-article:6132001 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:6132001 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:6132001 | pubmed:pagination | 61-9 | lld:pubmed |
| pubmed-article:6132001 | pubmed:dateRevised | 2007-11-14 | lld:pubmed |
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| pubmed-article:6132001 | pubmed:meshHeading | pubmed-meshheading:6132001-... | lld:pubmed |
| pubmed-article:6132001 | pubmed:year | 1983 | lld:pubmed |
| pubmed-article:6132001 | pubmed:articleTitle | Specific high-affinity binding sites for [3H]Ro 5-4864 in rat brain and kidney. | lld:pubmed |
| pubmed-article:6132001 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:6132001 | pubmed:publicationType | Research Support, U.S. Gov't, P.H.S. | lld:pubmed |
| pubmed-article:6132001 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
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