维拉帕米对二丁酰环磷酸腺苷引起的脂肪分解的影响。
Effects of verapamil on lipolysis due to dibutyryl cyclic AMP.
作者信息
Goko H, Takashima S, Shimizu S, Kagawa S, Matsuoka A
出版信息
Biochem J. 1984 May 15;220(1):321-4. doi: 10.1042/bj2200321.
The effects of verapamil, a calcium antagonist, on lipolysis in isolated rat adipocytes were studied. Verapamil (100 microM) potentiated lipolysis due to dibutyryl cyclic AMP (Bt2cAMP) at submaximal concentrations, with or without extracellular Ca2+. Lipolysis due to 0.5 mM-Bt2cAMP was potentiated by verapamil in a dose-dependent manner up to 200 microM, whereas at concentrations higher than 100 microM the stimulatory effect of verapamil was progressively diminished with or without extracellular Ca2+. Verapamil showed only an inhibitory effect on lipolysis due to adrenaline (0.1-10 microM) or 3-isobutyl-1-methylxanthine (IBMX; 25-200 microM). The stimulatory effect of verapamil on lipolysis due to Bt2cAMP was not blocked by alpha-adrenergic antagonists. These results suggest (i) that verapamil has a biphasic effect on lipolysis due to Bt2cAMP and only an inhibitory effect on that due to adrenaline or IBMX, and (ii) that extracellular Ca2+ or alpha-adrenergic receptors are not involved in the action of verapamil.
研究了钙拮抗剂维拉帕米对分离的大鼠脂肪细胞脂解作用的影响。维拉帕米（100微摩尔）在亚最大浓度下，无论有无细胞外钙离子，均可增强二丁酰环磷酸腺苷（Bt2cAMP）引起的脂解作用。维拉帕米以剂量依赖方式增强0.5毫摩尔-Bt2cAMP引起的脂解作用，直至200微摩尔，而在高于100微摩尔的浓度下，无论有无细胞外钙离子，维拉帕米的刺激作用均逐渐减弱。维拉帕米仅对肾上腺素（0.1 - 10微摩尔）或3 - 异丁基 - 1 - 甲基黄嘌呤（IBMX；25 - 200微摩尔）引起的脂解有抑制作用。维拉帕米对Bt2cAMP引起的脂解的刺激作用未被α - 肾上腺素能拮抗剂阻断。这些结果表明：（i）维拉帕米对Bt2cAMP引起的脂解有双相作用，而对肾上腺素或IBMX引起的脂解只有抑制作用；（ii）细胞外钙离子或α - 肾上腺素能受体不参与维拉帕米的作用。
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