Source:http://linkedlifedata.com/resource/pubmed/id/10344530
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
4
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| pubmed:dateCreated |
1999-7-23
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| pubmed:abstractText |
Numerous synthetic agonists selectively stimulate beta3-adrenoceptors (ARs). The endogenous catecholamines, noradrenaline and adrenaline, however, stimulate all the beta-AR subtypes, and no selective physiological agonist for beta3-ARs has been described so far. The aim of this study was to investigate whether any naturally occurring amine can stimulate selectively beta3-ARs. Since activation of lipolysis is a well-known beta-adrenergic function, the efficacy and potency of various biogenic amines were compared with those of noradrenaline, isoprenaline, and beta3-AR agonists 4-(-{[2-hydroxy-(3-chlorophenyl)ethyl]-amino} propyl)phenoxyacetate (BRL 37,344) and (R,R)-5-(2-{[2-(3-chlorophenyl )-2-hydroxyethyl]-amino} propyl)-1,3-benzo-dioxole-2,2-dicarboxylate (CL 316,243) by testing their lipolytic action in white fat cells. Five mammalian species were studied: rat, hamster and dog, in which selective beta-AR agonists act as full lipolytic agents, and guinea-pigs and humans, in which beta3-AR agonists are less potent activators of lipolysis. Several biogenic amines were inefficient (e.g. dopamine, tyramine and beta-phenylethylamine) while others (synephrine, phenylethanolamine, epinine) were partially active in stimulating lipolysis in all species studied. Their actions were inhibited by all the beta-AR antagonists tested, including those selective for beta1- or beta2-ARs. Octopamine was the only amine fully stimulating lipolysis in rat, hamster and dog fat cells, while inefficient in guinea-pig or human fat cells, like the beta3-AR agonists. In rat white fat cells, beta-AR antagonists inhibited the lipolytic effect of octopamine with a relative order of potency very similar to that observed against CL 316,243. Competitive antagonism of octopamine effect resulted in the following apparent pA2 [-log(IC50), where IC50 is the antagonist concentration eliciting half-maximal inhibition] values: 7.77 (bupranolol), 6.48 [3-(2-ethyl-phenoxy)-1[(1 S)-1,2,3,4-tetrahydronaphth-1-ylaminol]-(2S)2-propanol oxalate, SR 59230A, a beta3-selective antagonist], 6.30[erythro-D,L-1(7-lethylindan-4-yloxy)-3-isopropylamino-+ ++butan-2-ol, ICI 118,551, a beta2-selective antagonist] and 4.71 [(+/-)-[2-(3-carbomyl-4-hydroxyphenoxy)-ethylamino]-3-[4-(1- methyl-4-trifluoromethyl-2-imidazolyl)-phenoxy]2-propanolmethane sulphonate, CGP 20712A, a beta1-selective antagonist]. Octopamine had other properties in common with beta3-AR agonists: stimulation of oxygen consumption in rat brown fat cells and very low affinity in displacing [3H]CGP 12,177 binding to [beta1- or beta2-ARs in dog and rat adipocyte membranes. In Chinese hamster ovary (CHO) cells expressing human beta3-ARs, octopamine inhibited [125I]ICYP binding with only twofold less affinity than noradrenaline while it exhibited an affinity around 200-fold lower than noradrenaline in CHO cells expressing human beta1- or beta2-ARs. These data suggest that, among the biogenic amines metabolically related to catecholamines, octopamine can be considered as the most selective for beta3-ARs.
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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/3-(2-ethylphenoxy)-1-(1,2,3,4-tetrah...,
http://linkedlifedata.com/resource/pubmed/chemical/Adrenergic beta-Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/BRL 37344,
http://linkedlifedata.com/resource/pubmed/chemical/Biogenic Amines,
http://linkedlifedata.com/resource/pubmed/chemical/Bupranolol,
http://linkedlifedata.com/resource/pubmed/chemical/CGP 20712A,
http://linkedlifedata.com/resource/pubmed/chemical/CL 316243,
http://linkedlifedata.com/resource/pubmed/chemical/Dioxoles,
http://linkedlifedata.com/resource/pubmed/chemical/Ethanolamines,
http://linkedlifedata.com/resource/pubmed/chemical/ICI 118551,
http://linkedlifedata.com/resource/pubmed/chemical/Imidazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Iodine Radioisotopes,
http://linkedlifedata.com/resource/pubmed/chemical/Iodocyanopindolol,
http://linkedlifedata.com/resource/pubmed/chemical/Isoproterenol,
http://linkedlifedata.com/resource/pubmed/chemical/Norepinephrine,
http://linkedlifedata.com/resource/pubmed/chemical/Octopamine,
http://linkedlifedata.com/resource/pubmed/chemical/Propanolamines,
http://linkedlifedata.com/resource/pubmed/chemical/Propranolol,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, beta,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, beta-1,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, beta-2,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, beta-3
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| pubmed:status |
MEDLINE
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| pubmed:month |
Apr
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| pubmed:issn |
0028-1298
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| pubmed:author | |
| pubmed:issnType |
Print
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| pubmed:volume |
359
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| pubmed:owner |
NLM
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| pubmed:authorsComplete |
Y
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| pubmed:pagination |
310-21
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| pubmed:dateRevised |
2010-11-18
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| pubmed:meshHeading |
pubmed-meshheading:10344530-Adipose Tissue,
pubmed-meshheading:10344530-Adipose Tissue, Brown,
pubmed-meshheading:10344530-Adrenergic beta-Agonists,
pubmed-meshheading:10344530-Adult,
pubmed-meshheading:10344530-Animals,
pubmed-meshheading:10344530-Binding, Competitive,
pubmed-meshheading:10344530-Biogenic Amines,
pubmed-meshheading:10344530-Bupranolol,
pubmed-meshheading:10344530-CHO Cells,
pubmed-meshheading:10344530-Cricetinae,
pubmed-meshheading:10344530-Dioxoles,
pubmed-meshheading:10344530-Dogs,
pubmed-meshheading:10344530-Ethanolamines,
pubmed-meshheading:10344530-Female,
pubmed-meshheading:10344530-Gene Expression,
pubmed-meshheading:10344530-Guinea Pigs,
pubmed-meshheading:10344530-Humans,
pubmed-meshheading:10344530-Imidazoles,
pubmed-meshheading:10344530-Iodine Radioisotopes,
pubmed-meshheading:10344530-Iodocyanopindolol,
pubmed-meshheading:10344530-Isoproterenol,
pubmed-meshheading:10344530-Lipolysis,
pubmed-meshheading:10344530-Male,
pubmed-meshheading:10344530-Mammals,
pubmed-meshheading:10344530-Mesocricetus,
pubmed-meshheading:10344530-Norepinephrine,
pubmed-meshheading:10344530-Octopamine,
pubmed-meshheading:10344530-Oxygen Consumption,
pubmed-meshheading:10344530-Propanolamines,
pubmed-meshheading:10344530-Propranolol,
pubmed-meshheading:10344530-Rats,
pubmed-meshheading:10344530-Rats, Sprague-Dawley,
pubmed-meshheading:10344530-Receptors, Adrenergic, beta,
pubmed-meshheading:10344530-Receptors, Adrenergic, beta-1,
pubmed-meshheading:10344530-Receptors, Adrenergic, beta-2,
pubmed-meshheading:10344530-Receptors, Adrenergic, beta-3,
pubmed-meshheading:10344530-Species Specificity
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| pubmed:year |
1999
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| pubmed:articleTitle |
Selective activation of beta3-adrenoceptors by octopamine: comparative studies in mammalian fat cells.
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| pubmed:affiliation |
Institut National de la Santé et de la Recherche Médicale (INSERM), Unité 317, Institut Fédératif de Recherches 31, CHU Rangueil, Toulouse, France. carpene@rangueil.inserm.fr
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| pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
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