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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
1981-5-26
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pubmed:abstractText |
The presence of alpha 2-adrenergic receptors in membranes derived from human sc adipose tissue was directly demonstrated with a new alpha 2-selective ligand, [3H]yohimbine. Binding of this radiolabeled antagonist to adipocyte membranes was of high affinity (Kd = 3.9 +/- 2.4 nM) and saturable. Computer modelling of [3H]yohimbine saturation curves demonstrated that it binds to a homogeneous class of sites with a density of 145.0 +/- 33.8 fmol/mg protein. Adrenergic agonists competed with [3H]yohimbine in the order expected of alpha-receptors, and their binding was strongly influenced by guanine nucleotides. Competition of alpha-antagonists with this radioligand demonstrated yohimbine to be more potent than prazosin, indicative of alpha 2-receptors. Antagonist binding was unaffected by guanine nucleotides. Paired saturation curves in these adipocyte membranes with the alpha 2-selective [3H]yohimbine and the nonsubtype selective alpha-antagonist [3H]dihydroergocryptine demonstrated similar receptor concentrations. [3H]Dihydroergocryptine has been previously shown to label both alpha 3- and alpha 2-receptors with equal affinity. Therefore, these data indicate that the vast majority of alpha-receptors in human sc fat are of the alpha 2-subtype. [3H]Yohimbine with its alpha 2-selectivity and high specific binding will provide an excellent tool for the clinical investigation of human adipocyte alpha-receptor mechanisms in both normal and pathological states.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
AIM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Adrenergic alpha-Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, alpha,
http://linkedlifedata.com/resource/pubmed/chemical/Tritium,
http://linkedlifedata.com/resource/pubmed/chemical/Yohimbine
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
0021-972X
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
52
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
709-14
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:6110673-Adipose Tissue,
pubmed-meshheading:6110673-Adrenergic alpha-Antagonists,
pubmed-meshheading:6110673-Adult,
pubmed-meshheading:6110673-Aged,
pubmed-meshheading:6110673-Binding, Competitive,
pubmed-meshheading:6110673-Female,
pubmed-meshheading:6110673-Humans,
pubmed-meshheading:6110673-Kinetics,
pubmed-meshheading:6110673-Middle Aged,
pubmed-meshheading:6110673-Obesity,
pubmed-meshheading:6110673-Receptors, Adrenergic,
pubmed-meshheading:6110673-Receptors, Adrenergic, alpha,
pubmed-meshheading:6110673-Tritium,
pubmed-meshheading:6110673-Yohimbine
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pubmed:year |
1981
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pubmed:articleTitle |
alpha-Adrenergic receptors in human adipocyte membranes: direct determination by [3H]yohimbine binding.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
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