MK-801对NMDA刺激大鼠海马切片去甲肾上腺素释放的立体选择性拮抗作用。
Stereoselective antagonism of NMDA-stimulated noradrenaline release from rat hippocampal slices by MK-801.
作者信息
Lalies M, Middlemiss D N, Ransom R
机构信息
MSD Research Laboratories, Neuroscience Research Centre, Terlings Park, Harlow, U.K.
出版信息
Neurosci Lett. 1988 Sep 12;91(3):339-42. doi: 10.1016/0304-3940(88)90703-3.
N-Methyl-D-aspartate (NMDA)-stimulated [3H]noradrenaline release from rat hippocampal slices was blocked stereospecifically and non-competitively by MK-801 with the (+)-isomer achieving 50% blockade of 100 microM NMDA at 16 nM. The results indicate that MK-801 is the most potent NMDA antagonist yet described and that it blocks NMDA-stimulated neurotransmitter release by an action at the so-called 'phencyclidine (PCP) site'.
N-甲基-D-天冬氨酸（NMDA）刺激大鼠海马切片释放[3H]去甲肾上腺素的过程被MK-801立体特异性且非竞争性地阻断，其中（+）-异构体在16 nM时可对100 μM NMDA产生50%的阻断作用。结果表明，MK-801是迄今所描述的最有效的NMDA拮抗剂，并且它通过作用于所谓的“苯环利定（PCP）位点”来阻断NMDA刺激的神经递质释放。
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