| pubmed-article:2899462 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:2899462 | lifeskim:mentions | umls-concept:C0024299 | lld:lifeskim |
| pubmed-article:2899462 | lifeskim:mentions | umls-concept:C0010453 | lld:lifeskim |
| pubmed-article:2899462 | lifeskim:mentions | umls-concept:C0596981 | lld:lifeskim |
| pubmed-article:2899462 | lifeskim:mentions | umls-concept:C0597357 | lld:lifeskim |
| pubmed-article:2899462 | lifeskim:mentions | umls-concept:C0034785 | lld:lifeskim |
| pubmed-article:2899462 | lifeskim:mentions | umls-concept:C0001645 | lld:lifeskim |
| pubmed-article:2899462 | lifeskim:mentions | umls-concept:C0002334 | lld:lifeskim |
| pubmed-article:2899462 | lifeskim:mentions | umls-concept:C0033497 | lld:lifeskim |
| pubmed-article:2899462 | lifeskim:mentions | umls-concept:C0013081 | lld:lifeskim |
| pubmed-article:2899462 | lifeskim:mentions | umls-concept:C0237753 | lld:lifeskim |
| pubmed-article:2899462 | lifeskim:mentions | umls-concept:C0547047 | lld:lifeskim |
| pubmed-article:2899462 | pubmed:issue | 2 | lld:pubmed |
| pubmed-article:2899462 | pubmed:dateCreated | 1988-8-31 | lld:pubmed |
| pubmed-article:2899462 | pubmed:abstractText | We have used two different cultured cell lines--S49 lymphoma cells and BC3H-1 muscle cells--to examine the regulation of beta-adrenergic receptors by receptor antagonists. Rather than an increase ("up-regulation") of receptor number that such antagonists often produce, we found that certain beta-blockers elicit a decrease ("down-regulation") of beta-adrenergic receptors. Alprenolol and propranolol, but not sotalol or ICI 118,551, at concentrations of 10-100 nM down-regulated beta-adrenergic receptors 20-70% following 16-20 hours of treatment of S49 or BC3H-1 cells. Several observations suggest that this phenomenon depends upon beta-receptor interaction, including stereoselectivity [(-)-enantiomers more potent than (+)-enantiomers], blockade of the effect by ICI 118,551, absence of down-regulation of alpha-adrenergic receptors in BC3H-1 cells, and lack of a decrease in beta-adrenergic receptor-independent (forskolin-stimulated) cyclic AMP accumulation in S49 cells. The possibility of retained antagonist interfering with receptor measurement was precluded by the fact that the antagonist-induced decrease in receptor number required several hours incubation and occurred without a prominent change in receptor affinity. The ability of the beta-blockers to elicit down-regulation did not correlate with hydrophobicity of the drugs. Antagonist-induced down regulation of beta-adrenergic receptors did not occur in S49 lymphoma cells that lack the alpha-subunit of Gs, the guanine nucleotide-binding regulatory protein, thus implying a requirement for receptor-alpha s interaction in eliciting beta-receptor down-regulation.(ABSTRACT TRUNCATED AT 250 WORDS) | lld:pubmed |
| pubmed-article:2899462 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2899462 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2899462 | pubmed:language | eng | lld:pubmed |
| pubmed-article:2899462 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2899462 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:2899462 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2899462 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2899462 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2899462 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2899462 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2899462 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2899462 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2899462 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:2899462 | pubmed:month | Aug | lld:pubmed |
| pubmed-article:2899462 | pubmed:issn | 0009-7330 | lld:pubmed |
| pubmed-article:2899462 | pubmed:author | pubmed-author:InselP APA | lld:pubmed |
| pubmed-article:2899462 | pubmed:author | pubmed-author:HughesR JRJ | lld:pubmed |
| pubmed-article:2899462 | pubmed:author | pubmed-author:NEHAMSS | lld:pubmed |
| pubmed-article:2899462 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:2899462 | pubmed:volume | 63 | lld:pubmed |
| pubmed-article:2899462 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:2899462 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:2899462 | pubmed:pagination | 279-85 | lld:pubmed |
| pubmed-article:2899462 | pubmed:dateRevised | 2007-11-14 | lld:pubmed |
| pubmed-article:2899462 | pubmed:meshHeading | pubmed-meshheading:2899462-... | lld:pubmed |
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| pubmed-article:2899462 | pubmed:meshHeading | pubmed-meshheading:2899462-... | lld:pubmed |
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| pubmed-article:2899462 | pubmed:meshHeading | pubmed-meshheading:2899462-... | lld:pubmed |
| pubmed-article:2899462 | pubmed:meshHeading | pubmed-meshheading:2899462-... | lld:pubmed |
| pubmed-article:2899462 | pubmed:meshHeading | pubmed-meshheading:2899462-... | lld:pubmed |
| pubmed-article:2899462 | pubmed:meshHeading | pubmed-meshheading:2899462-... | lld:pubmed |
| pubmed-article:2899462 | pubmed:meshHeading | pubmed-meshheading:2899462-... | lld:pubmed |
| pubmed-article:2899462 | pubmed:meshHeading | pubmed-meshheading:2899462-... | lld:pubmed |
| pubmed-article:2899462 | pubmed:meshHeading | pubmed-meshheading:2899462-... | lld:pubmed |
| pubmed-article:2899462 | pubmed:meshHeading | pubmed-meshheading:2899462-... | lld:pubmed |
| pubmed-article:2899462 | pubmed:year | 1988 | lld:pubmed |
| pubmed-article:2899462 | pubmed:articleTitle | Certain beta-blockers can decrease beta-adrenergic receptor number: II. Down-regulation of receptor number by alprenolol and propranolol in cultured lymphoma and muscle cells. | lld:pubmed |
| pubmed-article:2899462 | pubmed:affiliation | Division of Pharmacology, University of California, San Diego, La Jolla. | lld:pubmed |
| pubmed-article:2899462 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:2899462 | pubmed:publicationType | Research Support, U.S. Gov't, P.H.S. | lld:pubmed |
| pubmed-article:2899462 | pubmed:publicationType | Research Support, U.S. Gov't, Non-P.H.S. | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:2899462 | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:2899462 | lld:pubmed |
