A-Rahim Y I, Rannels S L, Kimball S R, Beyer K H, Vesell E S
Department of Pharmacology, Pennsylvania State University, College of Medicine, Hershey 17033, USA.
Pharmacology. 1996 Oct;53(4):211-8. doi: 10.1159/000139432.
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.
在茶碱（1毫摩尔/升）刺激的离体大鼠脂肪细胞中，吡嗪甲酰胍（PZG）下调了脂肪分解和环磷酸腺苷（cAMP）浓度，这增加了PZG刺激脂肪组织胰岛素敏感性磷酸二酯酶的可能性。为了直接研究这一点，我们测量了PZG对大鼠脂肪细胞中磷酸二酯酶活性的影响。PZG（10微摩尔/升）以及胰岛素（0.1 - 1毫单位）增加了脂肪组织磷酸二酯酶活性，而茶碱则降低了该活性。我们还研究了PZG对灌注大鼠肝脏中糖异生和环磷酸腺苷的影响，结果显示PZG降低了糖异生和环磷酸腺苷浓度。
