Suzuki T, Sakai H, Ikari A, Takeguchi N
Department of Pharmaceutical Physiology, Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University, Toyama, 930-0194, Japan.
Jpn J Physiol. 2000 Jun;50(3):389-93. doi: 10.2170/jjphysiol.50.389.
The effects of 9,11-epithio-11,12-methano-thromboxane A(2) (STA(2)), a stable thromboxane A(2) analogue, and carbachol on colonic Ca(2+)-activated K(+) channels were studied. In indo-1-loaded single cells in isolated rat colonic crypts, both STA(2) (0.1 microM) and carbachol (10 microM) transiently increased intracellular free Ca(2+) concentration (Ca(2+)) by 136 and 155 nm, respectively. In whole-cell current-clamp experiments of the colonic crypt cells with Cl(-)-free solutions, carbachol (10 microM) hyperpolarized the cell by 19.7 mV, while STA(2) (0.1 microM) did not affect the membrane potential. In the isolated colonic mucosa that was permeabilized mucosally by a monovalent ionophore nystatin in the presence of a serosally directed K(+) gradient, carbachol (10 microM) transiently elicited K(+) current, but STA(2) (0.1 microM) did not. These results indicate that STA(2) elevates Ca(2+) in rat colonic crypt cells but does not activate basolateral Ca(2+)-activated K(+) channels.
研究了稳定的血栓素A2类似物9,11-环氧-11,12-甲撑血栓素A2(STA2)和卡巴胆碱对结肠钙激活钾通道的影响。在分离的大鼠结肠隐窝中加载indo-1的单细胞中,STA2(0.1微摩尔)和卡巴胆碱(10微摩尔)分别使细胞内游离钙浓度([Ca2+]i)瞬时增加136和155纳米。在使用无氯溶液的结肠隐窝细胞的全细胞电流钳实验中,卡巴胆碱(10微摩尔)使细胞超极化19.7毫伏,而STA2(0.1微摩尔)不影响膜电位。在存在浆膜侧钾离子梯度的情况下,通过单价离子载体制霉菌素使黏膜通透的分离结肠黏膜中,卡巴胆碱(10微摩尔)瞬时引发钾离子电流,但STA2(0.1微摩尔)则不能。这些结果表明,STA2可提高大鼠结肠隐窝细胞中的[Ca2+]i,但不激活基底外侧钙激活钾通道。