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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
4
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pubmed:dateCreated |
1993-6-4
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pubmed:abstractText |
1. The alpha 2-adrenoceptor antagonist capacities of two hydroxylated metabolites of yohimbine in man (10-OH-yohimbine and 11-OH-yohimbine) were investigated on the alpha 2-adrenoceptors of human platelets and adipocytes and compared to those of yohimbine. 2. Yohimbine and 11-OH-yohimbine exhibited similar alpha 2-adrenoceptor affinity in biological studies i.e. inhibition of adrenaline-induced platelet aggregation and inhibition of UK14304-induced antilipolysis in adipocytes. 3. Yohimbine and the two metabolites displaced [3H]-RX 821002 binding with equivalent affinities in platelet and adipocyte membranes with the following order of potency: yohimbine > 11-OH-yohimbine > 10-OH-yohimbine. However, when binding studies were carried out in binding buffer supplemented with 5% albumin, the apparent affinity of yohimbine was reduced about 10 fold and was similar to that of 11-OH-yohimbine. 4. Yohimbine and its metabolites were bound to different extents to plasma proteins, the bound fraction being 82%, 43% and 32% respectively for yohimbine, 11-OH-yohimbine and 10-OH-yohimbine. 5. These results show that the main hydroxylated metabolite of yohimbine in man (11-OH-yohimbine) possesses alpha 2-adrenoceptor antagonist properties. The discrepancies found in binding studies (i.e. 10 fold lower affinity of 11-OH-yohimbine than yohimbine for alpha 2-adrenoceptors but similar capacities in blocking biological alpha 2-adrenoceptor effects in cells) are attributable to the higher degree of binding of yohimbine to plasma protein.
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/8097957-13522708,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8097957-1618961,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8097957-1716906,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8097957-1885256,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8097957-1967647,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8097957-1976403,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8097957-2076728,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8097957-2076732,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8097957-2541903,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8097957-2552342,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8097957-2595649,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8097957-2906290,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8097957-3007161,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8097957-3022664,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8097957-3034620,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8097957-3653227,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8097957-3808301,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8097957-6140686,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8097957-6352483,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8097957-658127
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
0007-1188
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
108
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
927-32
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pubmed:dateRevised |
2009-11-18
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pubmed:meshHeading |
pubmed-meshheading:8097957-Adipose Tissue,
pubmed-meshheading:8097957-Adrenergic alpha-Agonists,
pubmed-meshheading:8097957-Adrenergic alpha-Antagonists,
pubmed-meshheading:8097957-Blood Platelets,
pubmed-meshheading:8097957-Blood Proteins,
pubmed-meshheading:8097957-Cell Membrane,
pubmed-meshheading:8097957-Dioxanes,
pubmed-meshheading:8097957-Epinephrine,
pubmed-meshheading:8097957-Humans,
pubmed-meshheading:8097957-Hydroxylation,
pubmed-meshheading:8097957-Idazoxan,
pubmed-meshheading:8097957-Lipolysis,
pubmed-meshheading:8097957-Male,
pubmed-meshheading:8097957-Platelet Aggregation,
pubmed-meshheading:8097957-Protein Binding,
pubmed-meshheading:8097957-Quinoxalines,
pubmed-meshheading:8097957-Yohimbine
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pubmed:year |
1993
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pubmed:articleTitle |
Alpha 2-adrenoceptor antagonist potencies of two hydroxylated metabolites of yohimbine.
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pubmed:affiliation |
INSERM U.317 Laboratoire de Pharmacologie Médicale et Clinique, Faculté de Médecine, Toulouse, France.
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pubmed:publicationType |
Journal Article,
In Vitro
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