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Electrophysiologically potent non-competitive glutamate antagonists at crayfish neuromuscular junctions are also potent inhibitors of [3H]MK801 binding to synaptic membranes from rat central nervous system

1994; Elsevier BV; Volume: 107; Issue: 1 Linguagem: Inglês

10.1016/1367-8280(94)90016-7

1878-1942

Mutsumi Maruyama, Keiko Takeda,

Analytical Chemistry and Sensors

This paper describes effects of non-competitive glutamate antagonists, also known as "glutamate open channel blockers", at crayfish neuromuscular junctions, on the binding of [3H]glutamate, [3H]CPP, [3H]AMPA, [3H]kainate and [3H]MK-801 to Triton-treated rat hippocampal synaptic membranes, and [3H]MK-801 to Triton-treated synaptic membranes from young rat spinal cord. The compounds tested were oxymatrine, theanine, diltiazem, chlorisondamine, tuberostemonine, trimethaphan, N2-dansyl-L-arginine-4-t-butylpiperidi amide (TI 233), (1RS,2SR)-5-methyl-1-phenyl-2-(3-piperid-inopropyl amino) hexane-1-ol (MLV-5860) and (4S,5R)-4-(2-methylpropyl)-3-[3-(perhydroazepin-1-yl)propyl]-5-phenyl-1, 3-oxazoline-2-one (MLV-6976). Among compounds tested, MLV-5860, MLV-6976 and TI 233 potently inhibited the binding of [3H]MK-801 to Triton-treated rat hippocampal synaptic membranes, but not that of other 3H-labelled ligands. The inhibitory potency of MLV-6976 and MLV-5860 on the binding of [3H]MK-801 was similar to that of MK-801. MLV-6976 could also inhibit the inhibitory potency was similar to MK-801. These results suggest that potent glutamate antagonists, acting as open channel blockers at crayfish neuromuscular junction, may have similar pharmacological properties to MK-801 at the mammalian central nervous system, but the reverse may not always be true.