Snell L D, Johnson K M
Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston 77550.
Synapse. 1989;3(2):129-35. doi: 10.1002/syn.890030204.
The nicotinic agonists dimethylphenylpiperazinium iodide (DMPP) and carbachol (CARB) as well as (-)nicotine [-)NIC) were tested alone and in combination with N-methyl-D-aspartate (NMDA) for their abilities to enhance the efflux of 3H-norepinephrine (NE) from slices of rat hippocampus. CARB and (-)NIC produced small, transient increases in NE efflux, while DMPP produced larger, longlasting increases. Inasmuch as the nicotinic antagonists mecamylamine (MECA) and hexamethonium (C6) did not consistently inhibit the increases in NE efflux produced by these agonists, the role of a nicotinic receptor in mediating these responses is uncertain. CARB and DMPP enhanced the ability of NMDA to stimulate NE release, while (-)NIC did not. MECA, but not C6, was found to selectively antagonize NMDA-stimulated NE release that did not appear to involve a nicotinic receptor. Binding studies indicated that MECA and the related nicotinic antagonist pempidine produced an inhibition of NMDA-stimulated NE release by an action at the PCP receptor that is known to be linked to the NMDA receptor-ionophore complex. These data suggest that the actions of these ganglionic blocking agents on excitatory responses in the hippocampus involve inhibition of excitatory amino acid as well as nicotinic receptors.
对烟碱激动剂碘化二甲基苯基哌嗪(DMPP)、卡巴胆碱(CARB)以及(-)尼古丁[(-)NIC]进行了单独测试,并测试了它们与N-甲基-D-天冬氨酸(NMDA)联合使用时增强大鼠海马切片中3H-去甲肾上腺素(NE)外流的能力。CARB和(-)NIC使NE外流产生小幅度的短暂增加,而DMPP则使NE外流产生大幅度的持久增加。由于烟碱拮抗剂美加明(MECA)和六甲铵(C6)并不能始终抑制这些激动剂所引起的NE外流增加,因此烟碱受体在介导这些反应中的作用尚不确定。CARB和DMPP增强了NMDA刺激NE释放的能力,而(-)NIC则没有。发现MECA而非C6能选择性拮抗NMDA刺激的NE释放,这似乎不涉及烟碱受体。结合研究表明,MECA和相关的烟碱拮抗剂潘必啶通过作用于已知与NMDA受体-离子通道复合物相关的苯环己哌啶受体来抑制NMDA刺激的NE释放。这些数据表明,这些神经节阻断剂对海马兴奋性反应的作用涉及抑制兴奋性氨基酸以及烟碱受体。