MECAMYLAMINE IS A SELECTIVE NON-COMPETITIVE ANTAGONIST OF N-METHYL-D-ASPARTATE-INDUCED AND ASPARTATE-INDUCED CURRENTS IN HORIZONTAL CELLS DISSOCIATED FROM THE CATFISH RETINA

MECAMYLAMINE IS A SELECTIVE NON-COMPETITIVE ANTAGONIST OF N-METHYL-D-ASPARTATE-INDUCED AND ASPARTATE-INDUCED CURRENTS IN HORIZONTAL CELLS DISSOCIATED FROM THE CATFISH RETINA
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DOI:
10.1016/0304-3940(88)90276-5
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发表时间:
1988-11-22
影响因子:
2.5
通讯作者:
CHRISTENSEN, BN
CHRISTENSEN, BN
中科院分区:
医学4区
文献类型:
--
作者:
ODELL, TJ;CHRISTENSEN, BN

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烟碱型乙酰胆碱通道阻断剂甲乙胺(MECA)和苯丙啶(PEMP)可阻断电压钳分离的视网膜锥对天冬氨酸(Asp)和N-甲基-D-天冬氨酸(NMDA)的水平反应,但对海人酸(Kainate)和奎尼定(Ququqate)诱发的电流影响不大。MECA对NMDA和Asp的浓度-反应曲线表明,MECA是NMDA和Asp反应的非竞争性抑制物。此外,MECA和PEMP阻断NMDA和Asp诱导的电流是高度电压敏感的。MECA对NMDA和Asp诱发电流的非竞争性和电压敏感性阻断提示MECA(和PEMP)阻断NMDA受体离子通道。
The nicotinic acetylcholine channel blockers mecamylamine (MECA) and pempidine (PEMP) blocked voltage-clamped isolated catfish retina cone horizontal responses to aspartate (Asp) and n-methyl-D-aspartate (NMDA) but had little effect on currents induced by kainate and quisqualate. Concentration-response curves for NMDA and Asp in the presence of MECA suggested that MECA was a non-competitive inhibitor of NMDA and Asp responses. Further, the MECA and PEMP block of NMDA and Asp-induced currents was highly voltage-sensitive. The non-competitive and voltage-sensitive block of NMDA and Asp-induced currents by MECA suggest that MECA (and PEMP) block the NMDA receptor ion channel.