Tojyo Y, Uchida M, Matsumoto Y
Department of Dental Pharmacology, School of Dentistry, Higashi-Nippon-Gakuen University, Hokkaido, Japan.
Jpn J Pharmacol. 1987 Dec;45(4):487-91. doi: 10.1254/jjp.45.487.
The effects of three calmodulin antagonists on rat parotid amylase release were investigated in vitro using a dispersed acinar cell preparation. The potent calmodulin antagonists, trifluoperazine (TFP) and N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7), inhibited both 1 microM isoproterenol (ISO)- and 1 mM dibutyryl cyclic AMP (DBcAMP)-stimulated amylase release in a dose-dependent manner at concentrations of 25-100 microM. The IC50 values for the ISO-stimulated amylase release were 22 microM with TFP and 42 microM with W-7, and the values for the DBcAMP-stimulated release were 25 microM and 48 microM, respectively. The weak calmodulin antagonist, N-(6-aminohexyl)-1-naphthalenesulfonamide (W-5), caused only slight inhibition at a concentration of 100 microM. These calmodulin antagonists only had a very small effect on the spontaneous release of lactate dehydrogenase. The results suggest that the calcium-calmodulin system may play a role in the exocytotic process of amylase release from the rat parotid gland.
使用分散的腺泡细胞制剂在体外研究了三种钙调蛋白拮抗剂对大鼠腮腺淀粉酶释放的影响。强效钙调蛋白拮抗剂三氟拉嗪（TFP）和N-（6-氨基己基）-5-氯-1-萘磺酰胺（W-7）在25-100微摩尔浓度下以剂量依赖方式抑制1微摩尔异丙肾上腺素（ISO）和1毫摩尔二丁酰环磷腺苷（DBcAMP）刺激的淀粉酶释放。ISO刺激的淀粉酶释放的IC50值，TFP为22微摩尔，W-7为42微摩尔；DBcAMP刺激的释放的值分别为25微摩尔和48微摩尔。弱钙调蛋白拮抗剂N-（6-氨基己基）-1-萘磺酰胺（W-5）在100微摩尔浓度下仅引起轻微抑制。这些钙调蛋白拮抗剂对乳酸脱氢酶的自发释放只有非常小的影响。结果表明，钙-钙调蛋白系统可能在大鼠腮腺淀粉酶释放的胞吐过程中起作用。
