rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
1989-12-7
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pubmed:abstractText |
alpha 2-Adrenergic receptors on NG 108 15 cell membranes were identified by [3H]rauwolscine binding: Bmax. = 661 +/- 81 fmol/mg of protein, Kd = 6.9 +/- 2.5 nM (mean +/- S.E.M., n = 6). On intact cells, stimulation of these receptors by (-)-adrenaline inhibited the prostaglandin-E1-stimulated adenylate cyclase activity by about 60%. The effect of (-)-adrenaline was pertussis-toxin-sensitive, indicating the involvement of an inhibitory G protein. (-)-Adrenaline/[3H]rauwolscine competition-binding experiments revealed that only 50% of the alpha 2 receptors were coupled to G proteins (i.e. displayed high agonist affinity). Pre-treatment of the cells with 20 microM-(-)-adrenaline provoked homologous desensitization of the alpha 2 receptors. The alpha 2-adrenergic response decreased after a time lag of about 2 h, to reach a minimum after 12 h. The bradykinin and muscarinic responses were not affected. The alpha 2-receptor concentration decreased without time lag. The high-agonist-affinity sites disappeared more rapidly (t1/2 = 42 min) than did the low-affinity uncoupled sites (t1/2 approx. 20 h). In contrast, pertussis-toxin-mediated [32P]ADP-ribosylation of inhibitory G proteins was unaffected by the pre-treatment. Pretreatment of intact NG 108 15 cells with 1 microM-phorbol 12-myristate 13-acetate (PMA) provoked a rapid decrease of the alpha 2-adrenergic response. The effect was nearly complete after 40 min. PMA also decreased the bradykinin response, suggesting a heterologous desensitization process. The alpha 2-receptor concentration, the (-)-adrenaline competition-binding curves and the pertussis- and cholera-toxin-mediated [32P]ADP-ribosylation of their respective G proteins were not affected.
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-14907713,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-2418346,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-2426098,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-2824982,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-2826414,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-2830256,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-2836188,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-2859516,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-2868003,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-2881298,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-2885739,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-2944002,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-2981397,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-2985920,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-2993919,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-3038126,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-3121596,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-3161729,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-3257691,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-3304132,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-33990,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-4040856,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-4318781,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-5432063,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-6254391,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2554886-6325124
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pubmed:language |
eng
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pubmed:journal |
|
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Adenylate Cyclase,
http://linkedlifedata.com/resource/pubmed/chemical/Alprostadil,
http://linkedlifedata.com/resource/pubmed/chemical/Bradykinin,
http://linkedlifedata.com/resource/pubmed/chemical/Carbachol,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclic AMP,
http://linkedlifedata.com/resource/pubmed/chemical/Epinephrine,
http://linkedlifedata.com/resource/pubmed/chemical/GTP-Binding Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, alpha,
http://linkedlifedata.com/resource/pubmed/chemical/Tetradecanoylphorbol Acetate,
http://linkedlifedata.com/resource/pubmed/chemical/Yohimbine
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pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
0264-6021
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
262
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
245-51
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pubmed:dateRevised |
2009-11-18
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pubmed:meshHeading |
pubmed-meshheading:2554886-Adenylate Cyclase,
pubmed-meshheading:2554886-Alprostadil,
pubmed-meshheading:2554886-Animals,
pubmed-meshheading:2554886-Binding, Competitive,
pubmed-meshheading:2554886-Bradykinin,
pubmed-meshheading:2554886-Carbachol,
pubmed-meshheading:2554886-Cells, Cultured,
pubmed-meshheading:2554886-Cyclic AMP,
pubmed-meshheading:2554886-Epinephrine,
pubmed-meshheading:2554886-GTP-Binding Proteins,
pubmed-meshheading:2554886-Neurons,
pubmed-meshheading:2554886-Receptors, Adrenergic, alpha,
pubmed-meshheading:2554886-Tetradecanoylphorbol Acetate,
pubmed-meshheading:2554886-Yohimbine
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pubmed:year |
1989
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pubmed:articleTitle |
Desensitization of alpha 2-adrenergic receptors in NG 108 15 cells by (-)-adrenaline and phorbol 12-myristate 13-acetate.
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pubmed:affiliation |
Department of Protein Chemistry, Vrije Universiteit Brussel, Belgium.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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