Ohata H, Maeda T, Momose K
Department of Pharmacology, School of Pharmaceutical Sciences, Showa University, Tokyo, Japan.
J Pharmacobiodyn. 1988 Jul;11(7):479-82. doi: 10.1248/bpb1978.11.479.
Inositol 1,4,5-trisphosphate (IP3) caused a contraction in skinned single smooth muscle cells from the guinea-pig taenia coli. The contractile response to IP3 was rapid (half time less than 5 s), concentration-dependent (0.01-10 microM, EC50; 0.1 microM) and also depended on the concentration of Ca2+ during preloading. IP3 induced a rapid 45Ca2+ release from the skinned single cells which were preloaded with 10(-6) M Ca2+. The contractile response caused by IP3 was not enhanced by simultaneous application of caffeine (25 mM). The inhibitory effect of procaine on IP3-induced contraction was less than that on caffeine-induced contraction. These results suggest that IP3 also plays an important role in the contractile response in smooth muscle cells from guinea-pig taenia coli and that the mechanism of Ca2+ release from intracellular storage sites by IP3 is different from that by caffeine.
肌醇1,4,5 -三磷酸(IP3)可引起豚鼠结肠带皮单个平滑肌细胞收缩。对IP3的收缩反应迅速(半衰期小于5秒),呈浓度依赖性(0.01 - 10微摩尔,半数有效浓度;0.1微摩尔),且还取决于预负荷期间的Ca2+浓度。IP3可诱导预先用10(-6) M Ca2+预负荷的带皮单个细胞快速释放45Ca2+。同时应用咖啡因(25毫摩尔)不会增强IP3引起的收缩反应。普鲁卡因对IP3诱导收缩的抑制作用小于对咖啡因诱导收缩的抑制作用。这些结果表明,IP3在豚鼠结肠带平滑肌细胞的收缩反应中也起重要作用,且IP3从细胞内储存位点释放Ca2+的机制与咖啡因不同。