Agmatine selectively blocks the N-methyl-D-aspartate subclass of glutamate receptor channels in rat hippocampal neurons.
作者： Donald J. Reis , Xian-Cheng Yang
DOI:
关键词: Agmatinase 、 Chemistry 、 Polyamine 、 Kainate receptor 、 Agmatine 、 NMDA receptor 、 Arginine decarboxylase 、 Biophysics 、 Patch clamp 、 Glutamate receptor 、 Biochemistry
摘要: We investigated in rat hippocampus neurons whether 4-(aminobutyl)guanidine (agmatine), formed by decarboxylation ofl-arginine arginine decarboxylase and metabolized to urea putrescine, can modulate the function of N -methyl-d-aspartate (NMDA) receptor channels. In cultured hippocampal studied whole-cell patch clamp, extracellular-applied agmatine produced a voltage- concentration-dependent block NMDA but not α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid nor kainate currents. Analysis voltage dependence suggests that binds at site located within channel pore with dissociation constant 952 μM 0 mV an electric distance 0.62. also tested effects several analogs. Arcaine (1,4-butyldiguanidine) similar voltage-dependent current, whereas putrescine (1,4-butyldiamine) had little effect, suggesting guanidine group is active moiety when blocking channel. Moreover, spermine (an endogenous polyamine) potentiated current even presence blocker or arcaine, guanidine-containing compounds arcaine interact binding different from spermine. Our results indicate selectively modulates subclass glutamate channels mediated interaction between pore. The support other data may as neurotransmitter/neuromodulator brain.
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