Joost H G, Göke B, Hasselblatt A
Arch Int Pharmacodyn Ther. 1983 May;263(1):155-63.
The effects of apomorphine, a partial agonist of dopamine, and of pimozide, an agent commonly used as an antagonist of dopamine, on insulin secretion from the perfused rat pancreas were studied. Apomorphine (10 and 100 microM) significantly reduced the insulin released in response to a stimulating glucose load. As judged from the perfusion pressure vasoconstriction could not account for the inhibitory action. The effect of apomorphine was not reversed by phentolamine infused to block alpha-receptors. Pimozide (1 microM) slightly weakened the inhibitory effect of apomorphine (10 microM) but failed to completely restore a normal secretion. An increase of the pimozide concentration (10 microM) revealed, however, that the agent itself reduced the glucose-induced insulin release. Thus a differentiation of dopamine agonistic and antagonistic effects could not be achieved with the aid of pimozide.
研究了多巴胺部分激动剂阿扑吗啡以及常用的多巴胺拮抗剂匹莫齐特对灌注大鼠胰腺胰岛素分泌的影响。阿扑吗啡(10微摩尔/升和100微摩尔/升)显著降低了对刺激性葡萄糖负荷反应时释放的胰岛素量。从灌注压力判断,血管收缩不能解释这种抑制作用。注入酚妥拉明阻断α受体并不能逆转阿扑吗啡的作用。匹莫齐特(1微摩尔/升)略微减弱了阿扑吗啡(10微摩尔/升)的抑制作用,但未能完全恢复正常分泌。然而,增加匹莫齐特浓度(10微摩尔/升)显示,该药物本身会降低葡萄糖诱导的胰岛素释放。因此,借助匹莫齐特无法区分多巴胺的激动和拮抗作用。