Merritt J E, Tomlinson S, Brown B L
Life Sci. 1983 Aug 29;33(9):889-93. doi: 10.1016/0024-3205(83)90628-8.
Several previous reports have indicated that a number of dopaminergic antagonists paradoxically inhibit prolactin secretion at micromolar concentrations. It is well known that some of these drugs, including pimozide and the phenothiazines, are inhibitors of calmodulin activity. Here we report that micromolar concentrations of several dopaminergic antagonists inhibit prolactin secretion from isolated rat anterior pituitary cells and calmodulin activity (calmodulin-activated cyclic GMP phosphodiesterase). Inhibition of calmodulin activity may thus, at least partially, explain the inhibitory effect of these drugs on prolactin secretion.
先前的几份报告表明,一些多巴胺能拮抗剂在微摩尔浓度下反而会抑制催乳素分泌。众所周知,其中一些药物,包括匹莫齐特和吩噻嗪类,是钙调蛋白活性的抑制剂。在此我们报告,几种多巴胺能拮抗剂的微摩尔浓度会抑制离体大鼠垂体前叶细胞的催乳素分泌以及钙调蛋白活性(钙调蛋白激活的环磷酸鸟苷磷酸二酯酶)。因此,钙调蛋白活性的抑制可能至少部分解释了这些药物对催乳素分泌的抑制作用。