Pinnock R D, Woodruff G N
Parke-Davis Neuroscience Research Unit, Addenbrookes Hospital Site, Cambridge, UK.
Neurosci Lett. 1994 May 19;172(1-2):175-8. doi: 10.1016/0304-3940(94)90690-4.
The pharmacology of the neurotensin response of dopamine-sensitive neurons in the substantia nigra compacta was examined by testing the effect of a novel neurotensin receptor antagonist, SR48692, on the response to neurotensin(8-13). Extracellular recordings of action potentials from neurons were made from coronal rat brain slices maintained in vitro. SR48692 was unable to antagonise the actions of neurotensin(8-13) until microM concentrations were applied. The equilibrium constant for SR48692 was 4.9 microM compared with low nM Ki values reported in binding experiments. The data suggests that the pharmacology of the neurotensin response in the rat substantia nigra may be different to that predicted from radioligand-binding studies in cell lines and brain homogenates.
通过测试新型神经降压素受体拮抗剂SR48692对神经降压素（8 - 13）反应的影响，研究了黑质致密部多巴胺敏感神经元的神经降压素反应药理学。在体外维持的大鼠脑冠状切片上，对神经元的动作电位进行细胞外记录。直到应用微摩尔浓度时，SR48692才能够拮抗神经降压素（8 - 13）的作用。SR48692的平衡常数为4.9微摩尔，而结合实验报道的Ki值为低纳摩尔。数据表明，大鼠黑质中神经降压素反应的药理学可能与细胞系和脑匀浆放射性配体结合研究预测的不同。
