The novel thermogenic beta-adrenergic agonist Ro 16-8714 increases the interscapular brown-fat beta-receptor-adenylate cyclase and the uncoupling-protein mRNA level in obese (fa/fa) Zucker rats.
In obese (fa/fa) rats both the total (-)-isoprenaline- and NaF-stimulated adenylate cyclase activities of interscapular brown-adipose-tissue (IBAT) plasma membranes were decreased as compared with lean rats by 40 and 38% respectively. An acute treatment with Ro 16-8714 increased (-)-isoprenaline- and NaF-stimulated adenylate cyclase activities by 2.5- and 2.0-fold respectively, and beta-adrenoceptor number 2.8-fold in obese rat IBAT, but it had no effect on these parameters in lean rats. It increased mRNA for mitochondrial uncoupling protein in both lean and obese rats to the same extent.
Muzzin
P
P
Département de Biochimie médicale, Centre médicale Universitaire, Genève, Switzerland.
Revelli
J P
JP
Ricquier
D
D
Meier
M K
MK
Assimacopoulos-Jeannet
F
F
Giacobino
J P
JP
D015078:2-Hydroxyphenethylamine / Q000031:analogs & derivatives / Q000494:pharmacology*; D000262:Adenylyl Cyclases / Q000378:metabolism*; D002001:Adipose Tissue, Brown / Q000187:drug effects / Q000201:enzymology* / Q000648:ultrastructure; D000318:Adrenergic beta-Agonists / Q000494:pharmacology*; D000818:Animals; D002352:Carrier Proteins; D002462:Cell Membrane / Q000201:enzymology; D005260:Female; D007473:Ion Channels; D008565:Membrane Proteins / Q000032:analysis*; D008928:Mitochondria / Q000032:analysis; D024101:Mitochondrial Proteins; D009765:Obesity / Q000201:enzymology; D010627:Phenethylamines / Q000494:pharmacology*; D012333:RNA, Messenger / Q000032:analysis; D051381:Rats; D011924:Rats, Zucker; D014475:Uncoupling Agents / Q000032:analysis; D000071256:Uncoupling Protein 1
D000318:Adrenergic beta-Agonists; D002352:Carrier Proteins; D007473:Ion Channels; D008565:Membrane Proteins; D024101:Mitochondrial Proteins; D010627:Phenethylamines; D012333:RNA, Messenger; D014475:Uncoupling Agents; D000071256:Uncoupling Protein 1; D015078:2-Hydroxyphenethylamine; C045606:4-(3-(bis(beta-hydroxyphenethyl)amino)butyl)benzamide; D000262:Adenylyl Cyclases