Connick J H, Addae J I, Nicholson C D, Stone T W
Department of Pharmacology, Organon Laboratories Ltd., Newhouse, Lanarkshire, U.K.
Eur J Pharmacol. 1992 Apr 22;214(2-3):169-73. doi: 10.1016/0014-2999(92)90115-k.
The sigma ligand 1,3-di-o-tolylguanidine (DTG) has been applied by microiontophoresis to neurones in the rat hippocampal slice and to neurones in the neocortex and hippocampus of rats anaesthetised with urethane. DTG depressed the excitatory responses of cells to both N-methyl-D-aspartate (NMDA) and quisqualate on a majority of the units tested, in no case causing an enhancement. Haloperidol had no consistent effect of its own and did not prevent the depressant effects of DTG. It is concluded that in the preparations used, DTG did not selectively modify neuronal sensitivity to NMDA.
西格玛配体1,3-二邻甲苯基胍(DTG)已通过微离子电泳法应用于大鼠海马切片中的神经元以及用氨基甲酸乙酯麻醉的大鼠新皮层和海马中的神经元。在大多数测试单元中,DTG抑制了细胞对N-甲基-D-天冬氨酸(NMDA)和quisqualate的兴奋性反应,在任何情况下都不会引起增强。氟哌啶醇本身没有一致的作用,也不能阻止DTG的抑制作用。得出的结论是,在所使用的制剂中,DTG没有选择性地改变神经元对NMDA的敏感性。