PMID- 16489409 OWN - NLM STAT- MEDLINE DCOM- 20131212 LR - 20060220 IS - 0371-0874 (Print) IS - 0371-0874 (Linking) VI - 58 IP - 1 DP - 2006 Feb 25 TI - [Effects of tetramethylpyrazine on large-conductance Ca(2)(+)-activated potassium channels in porcine coronary artery smooth muscle cells]. PG - 83-9 AB - The aim of the present study was to examine the effects of tetramethylpyrazine (TMP) on large-conductance Ca(2+)-activated potassium channels (BK(Ca) channels) in porcine coronary artery smooth muscle cells, in order to provide the experimental evidence for expounding the mechanism of TMP in dilating coronary artery. Cell-attached and inside-out single channel recording techniques were used to observe the effects of TMP on BK(Ca) channels as well as the effects after the cells were treated by protein kinase A (PKA) inhibitor or protein kinase G (PKG) inhibitor. In inside-out patch, TMP activated BK(Ca) channels by increasing open-state probability (N(Po)) and decreasing close time (Tc) in a concentration-dependent manner. TMP (0.73~8.07 mmol/L) in the bath solution increased N(Po) from (0.01+/-0.003) to (0.03+/-0.01)~(1.21+/-0.18) (P<0.01, n=10), and decreased Tc from (732.33+/-90.67) ms to (359.67+/-41.30) ~ (2.96+/-0.52) ms (P<0.01, n=10). These actions of TMP occurred even when the free Ca(2+) concentration in the bath was reduced to ~ 0 mmol/L. The specific inhibitors of PKA (H-89, 3 mumol/L) and PKG (KT-5823, 1 mumol/L) had no influence on the activation of TMP on BK(Ca) channels. These findings suggest that TMP can directly activate BK(Ca) channels in coronary artery smooth muscle, which probably is an important mechanism in dilating coronary artery. FAU - Yang, Yan-Yan AU - Yang YY AD - Institute of Myocardial Electrophysiology, Luzhou Medical College, Luzhou 646000, China. FAU - Yang, Yan AU - Yang Y FAU - Zeng, Xiao-Rong AU - Zeng XR FAU - Liu, Zhi-Fei AU - Liu ZF FAU - Cai, Fang AU - Cai F FAU - Li, Miao-Ling AU - Li ML FAU - Zhou, Wen AU - Zhou W FAU - Pei, Jie AU - Pei J LA - chi PT - English Abstract PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - China TA - Sheng Li Xue Bao JT - Sheng li xue bao : [Acta physiologica Sinica] JID - 20730130R RN - 0 (Potassium Channels, Calcium-Activated) RN - 0 (Pyrazines) RN - 0 (Vasodilator Agents) RN - V80F4IA5XG (tetramethylpyrazine) SB - IM MH - Animals MH - Coronary Vessels/*cytology MH - Muscle, Smooth, Vascular/cytology/*metabolism MH - Patch-Clamp Techniques MH - Potassium Channels, Calcium-Activated/*drug effects/physiology MH - Pyrazines/*pharmacology MH - Swine MH - Vasodilator Agents/*pharmacology EDAT- 2006/02/21 09:00 MHDA- 2013/12/18 06:00 CRDT- 2006/02/21 09:00 PHST- 2006/02/21 09:00 [pubmed] PHST- 2013/12/18 06:00 [medline] PHST- 2006/02/21 09:00 [entrez] PST - ppublish SO - Sheng Li Xue Bao. 2006 Feb 25;58(1):83-9.