Bolton T B, Lim S P
Department of Pharmacology & Clinical Pharmacology, St. George's Hospital Medical School, London, UK.
Z Kardiol. 1991;80 Suppl 7:73-7.
Contraction of smooth muscle by acetylcholine is mediated by activation of muscarinic receptors of which M2 and M3 subtypes are present in longitudinal muscle of guinea pig intestine. In single cells, muscarinic receptor activation evokes calcium release from stores which raises the internal free calcium concentration and causes opening of calcium-activated potassium channels. The rise in internal calcium suppresses the voltage-dependent inward calcium current. A third important effect is the opening of channels which cause depolarization of the membrane and so increase action potential discharge and contraction in the whole muscle. These channels were studied by voltage-clamp of single cells from longitudinal muscle of rabbit small intestine. They were found to be permeable to Na and K but not detectably permeable to Cl. They can pass Ca but the amount entering the cell is not sufficient to raise the internal calcium concentration appreciably.
乙酰胆碱引起的平滑肌收缩是由毒蕈碱受体激活介导的,豚鼠肠道纵肌中存在M2和M3亚型的毒蕈碱受体。在单细胞中,毒蕈碱受体激活引发钙从储存库中释放,这会提高细胞内游离钙浓度并导致钙激活钾通道开放。细胞内钙的升高会抑制电压依赖性内向钙电流。第三个重要作用是通道开放,这会导致细胞膜去极化,从而增加全肌的动作电位发放和收缩。这些通道通过对兔小肠纵肌单细胞进行电压钳研究。发现它们对Na和K通透,但对Cl几乎不通透。它们可以通过Ca,但进入细胞的量不足以显著提高细胞内钙浓度。