title: Studies on pyrazinoylguanidine. 4. Upregulation of phosphodiesterase activity in rat adipose tissue and downregulation of gluconeogenesis and adenosine 3',5'-monophosphate concentrations in perfused rat liver.
abstract: In isolated rat adipocytes stimulated with theophylline (1 mmol/l), pyrazinoylguanidine (PZG) downregulated both lipolysis and cyclic AMP concentrations, raising the possibility that PZG stimulates adipose insulin-sensitive phosphodiesterase. To investigate this directly, we measured PZG's effects on phosphodiesterase activity in rat adipocytes. PZG (10 mumol/l) as well as insulin (0.1-1 mU) increased adipose phosphodiesterase activity, whereas theophylline reduced it. Also investigated were PZG's effects on gluconeogenesis and cyclic AMP in perfused rat liver where PZG decreased gluconeogenesis and cyclic AMP concentrations.
authors.affiliation: Department of Pharmacology, Pennsylvania State University, College of Medicine, Hershey 17033, USA.
authors.forename: Y I
authors.initials: YI
authors.lastname: A-Rahim
authors.forename: S L
authors.initials: SL
authors.lastname: Rannels
authors.forename: S R
authors.initials: SR
authors.lastname: Kimball
authors.forename: K H
authors.initials: KH
authors.lastname: Beyer
authors.forename: E S
authors.initials: ES
authors.lastname: Vesell
mesh_terms: D017667:Adipocytes / Q000187:drug effects / Q000378:metabolism; D000273:Adipose Tissue / Q000187:drug effects / Q000201:enzymology*; D000818:Animals; D002462:Cell Membrane / Q000187:drug effects / Q000201:enzymology; D000242:Cyclic AMP / Q000096:biosynthesis*; D015536:Down-Regulation / Q000187:drug effects; D005943:Gluconeogenesis / Q000187:drug effects*; D006146:Guanidines / Q000494:pharmacology*; D007004:Hypoglycemic Agents / Q000494:pharmacology*; D066298:In Vitro Techniques; D008099:Liver / Q000187:drug effects / Q000201:enzymology / Q000378:metabolism*; D008297:Male; D010726:Phosphodiesterase Inhibitors / Q000494:pharmacology; D010727:Phosphoric Diester Hydrolases / Q000378:metabolism*; D011719:Pyrazines / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013806:Theophylline / Q000494:pharmacology; D015854:Up-Regulation / Q000187:drug effects
chemical_list: D006146:Guanidines; D007004:Hypoglycemic Agents; D010726:Phosphodiesterase Inhibitors; D011719:Pyrazines; C056104:2-pyrazinoylguanidine; D013806:Theophylline; D000242:Cyclic AMP; D010727:Phosphoric Diester Hydrolases