Zhu Hai-Lei, Hirst G David S, Ito Yushi, Teramoto Noriyoshi
Department of Pharmacology, Graduate School of Medical Sciences, Kyushu University, Higashi Ward, Fukuoka, Japan.
Br J Pharmacol. 2005 Sep;146(1):129-38. doi: 10.1038/sj.bjp.0706295.
We have investigated whether the activation of cAMP- and cGMP-dependent pathways modifies the properties of voltage-dependent Ba(2+) currents (I(Ba)) recorded from guinea-pig gastric myocytes using patch-clamp techniques. All experiments were carried on single smooth muscle cells, dispersed from the circular layer of the guinea-pig gastric antrum. Both dibutyryl cAMP (db-cAMP, 0.1-1 mM), a membrane-permeable ester of cAMP, and isoproterenol, a selective beta-stimulant, inhibited I(Ba) in a concentration-dependent manner. Forskolin, but not dideoxy-forskolin, an inactive isomer of forskolin, inhibited the peak amplitude of I(Ba). In the presence of either Rp-cAMP or the PKA (cAMP-dependent protein kinase) inhibitor peptide 5-24 (PKA-IP), neither forskolin nor db-cAMP inhibited I(Ba). After establishing a conventional whole-cell recording, the peak amplitude of I(Ba) gradually decreased when the catalytic subunit of PKA was included in the pipette. The further application of Rp-cAMP reversibly enhanced I(Ba). Sodium nitroprusside (0.1-1 mM) and 8-Br-cGMP (0.1-1 mM) also inhibited I(Ba) in a concentration-dependent manner. The inhibitory effects of forskolin or db-cAMP on I(Ba) were not significantly changed by pretreatment with a cGMP-dependent protein kinase (PKG) inhibitor. Similarly, the inhibitory actions of 8-Br-cGMP on I(Ba) were not modified by PKA-IP. The membrane-permeable cyclic nucleotides db-cAMP and 8-Br-cGMP caused little shift of the voltage dependence of the steady-state inactivation and reactivation curves. Neither of the membrane-permeable cyclic nucleotides db-cAMP or 8-Br-cGMP had additive inhibitory effects on I(Ba). These results indicate that two distinct cyclic nucleotide-dependent pathways are present in the guinea-pig gastric antrum, and that both inhibited I(Ba) in an independent manner.
我们利用膜片钳技术研究了环磷酸腺苷(cAMP)和环磷酸鸟苷(cGMP)依赖性途径的激活是否会改变豚鼠胃肌细胞中记录到的电压依赖性钡电流(I(Ba))的特性。所有实验均在从豚鼠胃窦环形肌层分离出的单个平滑肌细胞上进行。环磷酸腺苷的膜透性酯二丁酰环磷腺苷(db-cAMP,0.1 - 1 mM)和选择性β激动剂异丙肾上腺素均以浓度依赖性方式抑制I(Ba)。福斯可林可抑制I(Ba)的峰值幅度,而其无活性异构体双脱氧福斯可林则无此作用。在存在Rp-cAMP或蛋白激酶A(cAMP依赖性蛋白激酶)抑制剂肽5 - 24(PKA-IP)的情况下,福斯可林和db-cAMP均不抑制I(Ba)。在建立传统的全细胞记录后,当移液器中包含蛋白激酶A的催化亚基时,I(Ba)的峰值幅度逐渐降低。进一步应用Rp-cAMP可使I(Ba)可逆性增强。硝普钠(0.1 - 1 mM)和8-溴环磷酸鸟苷(0.1 - 1 mM)也以浓度依赖性方式抑制I(Ba)。用cGMP依赖性蛋白激酶(PKG)抑制剂预处理后,福斯可林或db-cAMP对I(Ba)的抑制作用无明显变化。同样,PKA-IP也不改变8-溴环磷酸鸟苷对I(Ba)的抑制作用。膜透性环核苷酸db-cAMP和8-溴环磷酸鸟苷对稳态失活和再激活曲线的电压依赖性几乎没有影响。膜透性环核苷酸db-cAMP或8-溴环磷酸鸟苷对I(Ba)均无相加抑制作用。这些结果表明,豚鼠胃窦中存在两种不同的环核苷酸依赖性途径,且二者均以独立方式抑制I(Ba)。