CGP 37849

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CGP 37849 是一种有效的竞争性口服活性 N-甲基-D-天冬氨酸 (NMDA) 受体拮抗剂。CGP 37849 是啮齿动物的抗惊厥药，具有抗抑郁和抗焦虑作用。

CGP 37849 is a potent, competitive and orally active N-methyl-D-aspartate (NMDA) receptor antagonist. CGP 37849 is an anticonvulsant in rodents and has antidepressant and anxiolytic-like effects.

In the hippocampal slice in vitro, CGP 37849 selectively and reversibly antagonizes NMDA-evoked increases in CA1 pyramidal cell firing rate. In slices bathed in medium containing low Mg2+ levels, concentrations of CGP 37849 up to 10 μM suppresses burst firing evoked in CA1 neurones by stimulation of Schaffer collateral-commissural fibres without affecting the magnitude of the initial population spike.

CGP 37849 potently (Ki of 220 nM) and competitively inhibits NMDA-sensitive l-[3H]-glutamate binding to postsynaptic density (PSD) fractins from rat brain. CGP 37849 inhibits the binding of the selective NMDA receptor antagonist, [3H]-(±)-3-(2-carboxypiperazin-4-yl)propyl-1-phosphonate (CPP), with a Ki of 35 nM.In vivo, oral administration to rats of CGP 37849 selectively blocks firing in hippocampal neurones induced by ionophoretically-applied NMDA, without affecting the responses to quisqualate or kainate.Oral administration to mice of CGP 37849 suppresses maximal electroshock-induced seizures in mice with an ED50 of 21 mg/kg.

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Membrane Transporter/Ion Channel

iGluR

iGluR | NMDAR

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127910-31-0

209.14

C6H12NO5P

>98% (HPLC)

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C\C(CP(O)(O)=O)=C/C(N)C(O)=O

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(-20℃)

With Ice Pack

≥ 2 years