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CGP 37849

CAS No. : 127910-31-0

MCE 站：CGP 37849

产品活性：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。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：iGluR

In Vitro: 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.

In Vivo: CGP 37849 potently (K_i 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 K_i 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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