| pubmed-article:6119625 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:6119625 | lifeskim:mentions | umls-concept:C0020792 | lld:lifeskim |
| pubmed-article:6119625 | lifeskim:mentions | umls-concept:C0085979 | lld:lifeskim |
| pubmed-article:6119625 | lifeskim:mentions | umls-concept:C0023688 | lld:lifeskim |
| pubmed-article:6119625 | lifeskim:mentions | umls-concept:C0445604 | lld:lifeskim |
| pubmed-article:6119625 | lifeskim:mentions | umls-concept:C1709793 | lld:lifeskim |
| pubmed-article:6119625 | lifeskim:mentions | umls-concept:C0056670 | lld:lifeskim |
| pubmed-article:6119625 | pubmed:issue | 4 | lld:pubmed |
| pubmed-article:6119625 | pubmed:dateCreated | 1982-3-22 | lld:pubmed |
| pubmed-article:6119625 | pubmed:abstractText | (+/-)[125Iodo] cyanopindolol (ICYP) is a radioligand which binds with an extraordinarily high affinity and specificity to beta-adrenoceptors. In contrast to (+/-) [125Ido]-hydroxybenzylpindolol (IHYP), the new ligand has neither affinity to alpha-nor to 5-HT-receptors. The dissociation constants of ICYP for beta- adrenoceptors in various tissues range from 27 to 40 pM, thereby exceeding the affinity of IHYP by a factor of approximately 3. ICYP does not discriminate between beta 1- and beta 2-adrenoceptors. Therefore, the densities of the two receptor subtypes can be determined from competition curves of ICYP by drugs previously found to show in vitro selectivity for beta 1-adrenoceptors. The guinea pig left ventricle contains only beta 1-adrenoceptors, whereas in a lung tissue, the ratio of beta 1-to beta 2-adrenoceptors is 1 to 4. The calculated affinities of five beta 1-selective antagonists for beta 1-adrenoceptors were nearly identical in the ventricle and the lung. Kinetic studies of ICYP binding to guinea pig lung membranes indicated that the dissociation reaction consists of two components, a fast process (t 1/2 = 9 min) and a slower process (t 1/2 = 8.8 h). A mathematical treatment revealed two possibilities of interpretation: 1. Two forms of the receptor exist which are interconvertible. 2. The (+)- and (-)- enantiomers of ICYP dissociate with different rate constants. The low dissociation constant of ICYP in combination with its high specific radioactivity (2175 Ci mmole -1) allows binding studies to be carried out with small protein and ligand concentrations, e.g. 3 microgram protein per assay in guinea pig lung membranes. | lld:pubmed |
| pubmed-article:6119625 | pubmed:language | eng | lld:pubmed |
| pubmed-article:6119625 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:6119625 | pubmed:citationSubset | IM | lld:pubmed |
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| pubmed-article:6119625 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:6119625 | pubmed:issn | 0028-1298 | lld:pubmed |
| pubmed-article:6119625 | pubmed:author | pubmed-author:WagnerHH | lld:pubmed |
| pubmed-article:6119625 | pubmed:author | pubmed-author:EngelGG | lld:pubmed |
| pubmed-article:6119625 | pubmed:author | pubmed-author:HoyerDD | lld:pubmed |
| pubmed-article:6119625 | pubmed:author | pubmed-author:BertholdRR | lld:pubmed |
| pubmed-article:6119625 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:6119625 | pubmed:volume | 317 | lld:pubmed |
| pubmed-article:6119625 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:6119625 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:6119625 | pubmed:pagination | 277-85 | lld:pubmed |
| pubmed-article:6119625 | pubmed:dateRevised | 2003-11-14 | lld:pubmed |
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| pubmed-article:6119625 | pubmed:meshHeading | pubmed-meshheading:6119625-... | lld:pubmed |
| pubmed-article:6119625 | pubmed:year | 1981 | lld:pubmed |
| pubmed-article:6119625 | pubmed:articleTitle | (+/-)[125Iodo] cyanopindolol, a new ligand for beta-adrenoceptors: identification and quantitation of subclasses of beta-adrenoceptors in guinea pig. | lld:pubmed |
| pubmed-article:6119625 | pubmed:publicationType | Journal Article | lld:pubmed |
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