pubmed-article:2835476 | rdf:type | pubmed:Citation | lld:pubmed |
pubmed-article:2835476 | lifeskim:mentions | umls-concept:C0007600 | lld:lifeskim |
pubmed-article:2835476 | lifeskim:mentions | umls-concept:C0040300 | lld:lifeskim |
pubmed-article:2835476 | lifeskim:mentions | umls-concept:C0540641 | lld:lifeskim |
pubmed-article:2835476 | lifeskim:mentions | umls-concept:C1167622 | lld:lifeskim |
pubmed-article:2835476 | lifeskim:mentions | umls-concept:C0231491 | lld:lifeskim |
pubmed-article:2835476 | lifeskim:mentions | umls-concept:C0332256 | lld:lifeskim |
pubmed-article:2835476 | lifeskim:mentions | umls-concept:C0449560 | lld:lifeskim |
pubmed-article:2835476 | pubmed:issue | 2 | lld:pubmed |
pubmed-article:2835476 | pubmed:dateCreated | 1988-6-16 | lld:pubmed |
pubmed-article:2835476 | pubmed:abstractText | The affinities of 34 adrenergic antagonists for alpha-2 adrenergic receptors were determined from homogenate radioligand binding studies using [3H]yohimbine and [3H]rauwolscine. It has been suggested that alpha-2 adrenergic receptors can be subdivided into alpha-2A and alpha-2B subtypes. Oxymetazoline is selective for alpha-2A receptors, whereas prazosin is alpha-2B selective. Five different tissues were used, each of which has only one of the two subtypes: human platelet (alpha-2A), HT29 cell line (alpha-2A), human cerebral cortex (alpha-2A), neonatal rat lung (alpha-2B), and NG108-15 cell line (alpha-2B). The drug affinities were highly correlated when alpha-2A tissues were compared with alpha-2A tissues (r = 0.97 to 0.98) or when the two alpha-2B tissues were compared (r = 0.99). By contrast, comparison of an alpha-2A tissue with an alpha-2B tissue resulted in poor correlations (r = 0.77 to -0.87). Three new subtype selective drugs were identified among these drugs on the basis of at least a 10-fold greater affinity for one subtype. All three were selective for the alpha-2B subtype: ARC-239 (100-fold selective), chlorpromazine (18-fold selective), and 7-hydroxychlorpromazine (17-fold selective). These studies, by demonstrating distinct pharmacological profiles for the two alpha-2 adrenergic receptor subtypes in several different tissues, further support the existence and definition of these subtypes. The identification of a cell line for each subtype should be useful in the further study of alpha-2 adrenergic receptor subtypes. | lld:pubmed |
pubmed-article:2835476 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:2835476 | pubmed:language | eng | lld:pubmed |
pubmed-article:2835476 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:2835476 | pubmed:citationSubset | IM | lld:pubmed |
pubmed-article:2835476 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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pubmed-article:2835476 | pubmed:status | MEDLINE | lld:pubmed |
pubmed-article:2835476 | pubmed:month | May | lld:pubmed |
pubmed-article:2835476 | pubmed:issn | 0022-3565 | lld:pubmed |
pubmed-article:2835476 | pubmed:author | pubmed-author:BylundD BDB | lld:pubmed |
pubmed-article:2835476 | pubmed:author | pubmed-author:MurphyT JTJ | lld:pubmed |
pubmed-article:2835476 | pubmed:author | pubmed-author:Ray-PrengerCC | lld:pubmed |
pubmed-article:2835476 | pubmed:issnType | Print | lld:pubmed |
pubmed-article:2835476 | pubmed:volume | 245 | lld:pubmed |
pubmed-article:2835476 | pubmed:owner | NLM | lld:pubmed |
pubmed-article:2835476 | pubmed:authorsComplete | Y | lld:pubmed |
pubmed-article:2835476 | pubmed:pagination | 600-7 | lld:pubmed |
pubmed-article:2835476 | pubmed:dateRevised | 2007-11-14 | lld:pubmed |
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pubmed-article:2835476 | pubmed:year | 1988 | lld:pubmed |
pubmed-article:2835476 | pubmed:articleTitle | Alpha-2A and alpha-2B adrenergic receptor subtypes: antagonist binding in tissues and cell lines containing only one subtype. | lld:pubmed |
pubmed-article:2835476 | pubmed:affiliation | Department of Pharmacology, School of Medicine, University of Missouri, Columbia. | lld:pubmed |
pubmed-article:2835476 | pubmed:publicationType | Journal Article | lld:pubmed |
pubmed-article:2835476 | pubmed:publicationType | Research Support, U.S. Gov't, P.H.S. | lld:pubmed |
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