Document Detail

SR59230A blocks beta3-adrenoceptor-linked modulation of upcoupling protein-1 and leptin in rat brown adipocytes.
MedLine Citation:
PMID:  9718277     Owner:  NLM     Status:  MEDLINE    
Experimental evidence suggests that, by stimulating energy expenditure in brown fat, selective beta3-adrenoceptor agonists can reduce body weight in obese rodents. In order to investigate further the physiological role of beta3-adrenoceptors in brown adipocytes, we analysed the effects of selective beta3-adrenoceptor agonists and antagonists on uncoupling protein-1 and leptin gene expression in culture-differentiated brown fat cells. Our main findings were that: (i) the leptin gene is expressed in brown adipocytes; (ii) the selective beta3-adrenoceptor agonist, N[(2S)-7-carbethoxy-1,2,3,4-tetrahydronaphth-2-yl]-(2R)-2-hydroxy- 2-(3-chlorophenil)ethanamine hydrochloride (SR58611A), inhibits leptin gene while inducing uncoupling protein-1 gene expression; (iii) these opposite effects of SR58611A are antagonized by the selective beta3-adrenoceptor antagonist, SS-enantiomer 3-(2-ethylphenoxy)-1-(1S),2,3,4-tetrahydronaphth-1-ylamin ol]-(2S)-2-propanol oxalate (SR59230A), but not by the selective beta1-adrenoceptor antagonist (+/-)-[2-(3-carbamoyl-4-hydroxyphenoxy)-ethylamino]-3-[4(1-methyl- 4-trifluoromethyl-2-imidazolyl)-phenoxy]-2 propanol (CGP20712A); and (iv) these effects are due to increased cyclic AMP levels. These results confirm by means of a different experimental approach that beta3-adrenoceptors play a central role in controlling the expression of genes that are important for brown fat function.
C Tonello; L Dioni; L Briscini; E Nisoli; M O Carruba
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  European journal of pharmacology     Volume:  352     ISSN:  0014-2999     ISO Abbreviation:  Eur. J. Pharmacol.     Publication Date:  1998 Jul 
Date Detail:
Created Date:  1998-10-26     Completed Date:  1998-10-26     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  1254354     Medline TA:  Eur J Pharmacol     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  125-9     Citation Subset:  IM    
Centre for Study and Research on Obesity, Department of Pharmacology, School of Medicine, Ospedale L. Sacco, Milan University, Italy.
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MeSH Terms
Adipocytes / drug effects,  metabolism
Adipose Tissue, Brown / cytology,  drug effects*,  metabolism
Adrenergic beta-Agonists / pharmacology*
Base Sequence
Carrier Proteins / metabolism*
Cells, Cultured
DNA Primers
Ion Channels
Membrane Proteins / metabolism*
Mitochondrial Proteins
Propanolamines / pharmacology*
Proteins / metabolism*
Rats, Sprague-Dawley
Receptors, Adrenergic, beta / drug effects
Receptors, Adrenergic, beta-3
Reverse Transcriptase Polymerase Chain Reaction
Reg. No./Substance:
0/Adrenergic beta-Agonists; 0/Carrier Proteins; 0/DNA Primers; 0/Ion Channels; 0/Leptin; 0/Membrane Proteins; 0/Mitochondrial Proteins; 0/Propanolamines; 0/Proteins; 0/Receptors, Adrenergic, beta; 0/Receptors, Adrenergic, beta-3; 0/SR 59230A; 0/mitochondrial uncoupling protein

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