| pubmed-article:23392 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:23392 | lifeskim:mentions | umls-concept:C0086418 | lld:lifeskim |
| pubmed-article:23392 | lifeskim:mentions | umls-concept:C0020792 | lld:lifeskim |
| pubmed-article:23392 | lifeskim:mentions | umls-concept:C0005821 | lld:lifeskim |
| pubmed-article:23392 | lifeskim:mentions | umls-concept:C0034784 | lld:lifeskim |
| pubmed-article:23392 | lifeskim:mentions | umls-concept:C0012290 | lld:lifeskim |
| pubmed-article:23392 | lifeskim:mentions | umls-concept:C1167622 | lld:lifeskim |
| pubmed-article:23392 | pubmed:issue | 2 | lld:pubmed |
| pubmed-article:23392 | pubmed:dateCreated | 1978-3-29 | lld:pubmed |
| pubmed-article:23392 | pubmed:abstractText | Binding of [(3)H]dihydroergocryptine to platelet lysates appears to have all the characteristics of binding to alpha-adrenergic receptors. At 25 degrees C binding reaches equilibrium within 20 min and is reversible upon addition of excess phentolamine. Binding is saturable with 183+/-22 fmol of [(3)H]dihydroergocryptine bound per mg of protein at saturation, corresponding to 220+/-26 sites per platelet. Kinetic and equilibrium studies indicate the dissociation constant of [(3)H]dihydroergocryptine for the receptors is 1-3 nM. The specificity of the binding sites is typical of an alpha-adrenergic receptor. Catecholamine agonists compete for occupancy of the [(3)H]dihydroergocryptine binding sites with an order of potency (-)epinephrine> (-)norepinephrine>> (-)isoproterenol. Stereospecificity was demonstrated inasmuch as the (+)isomers of epinephrine and norepinephrine were 10-20-fold less potent than the (-)isomers. The potent alpha-adrenergic antagonists phentolamine, phenoxybenzamine, and yohimbine competed potently for the sites, whereas beta-antagonists such as propranolol and dichlorisoproterenol were quite weak. Dopamine and serotonin competed only at high concentrations (0.1 mM). The [(3)H]dihydroergocryptine binding sites could also be demonstrated in intact platelets where they displayed comparable specificity, stereospecificity, and saturability. Saturation binding studies with the intact platelets indicated 220+/-45 receptors per platelet, in good agreement with the value derived from studies with platelet lysates. Ability of alpha-adrenergic agonists to inhibit adenylate cyclase and of alpha-adrenergic antagonists to antagonize this inhibitory effect directly paralleled ability to interact with the [(3)H]dihydroergocryptine binding sites. These data demonstrate the feasibility of directly studying alpha-adrenergic receptor binding sites in human platelets with [(3)H]dihydroergocryptine. | lld:pubmed |
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| pubmed-article:23392 | pubmed:language | eng | lld:pubmed |
| pubmed-article:23392 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:23392 | pubmed:citationSubset | AIM | lld:pubmed |
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| pubmed-article:23392 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:23392 | pubmed:month | Feb | lld:pubmed |
| pubmed-article:23392 | pubmed:issn | 0021-9738 | lld:pubmed |
| pubmed-article:23392 | pubmed:author | pubmed-author:LefkowitzR... | lld:pubmed |
| pubmed-article:23392 | pubmed:author | pubmed-author:WilliamsL TLT | lld:pubmed |
| pubmed-article:23392 | pubmed:author | pubmed-author:NewmanK DKD | lld:pubmed |
| pubmed-article:23392 | pubmed:author | pubmed-author:BishopricN... | lld:pubmed |
| pubmed-article:23392 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:23392 | pubmed:volume | 61 | lld:pubmed |
| pubmed-article:23392 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:23392 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:23392 | pubmed:pagination | 395-402 | lld:pubmed |
| pubmed-article:23392 | pubmed:dateRevised | 2009-11-18 | lld:pubmed |
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| pubmed-article:23392 | pubmed:year | 1978 | lld:pubmed |
| pubmed-article:23392 | pubmed:articleTitle | Identification of alpha-adrenergic receptors in human platelets by [3H]dihydroergocryptine binding. | lld:pubmed |
| pubmed-article:23392 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:23392 | pubmed:publicationType | In Vitro | lld:pubmed |
| pubmed-article:23392 | pubmed:publicationType | Research Support, U.S. Gov't, P.H.S. | lld:pubmed |
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