127910-31-0
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基本信息
CGP 37849
CGP-37849
CGP37849
dl-2-amino-4-methyl-5-phosphono-3-*pentenoic acid
(E)-2-Amino-4-methyl-5-phosphonopent-3-enoic acid
(3E)-2-Amino-4-methyl-5-phosphono-3-pentanoic acid
(E)-(±)-2-AMINO-4-METHYL-5-PHOSPHONO-3-PENTENOIC ACID
3-Pentenoic acid, 2-amino-4-methyl-5-phosphono-, (3E)-
(E)-(+/-)-2-AMINO-4-METHYL-5-PHOSPHONO-3-PENTENOIC ACID
物理化学性质
常见问题列表
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 Mg 2+ 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 (
K
i
of 220 nM) and competitively inhibits NMDA-sensitive l-[
3
H]-glutamate binding to postsynaptic density (PSD) fractins from rat brain. CGP 37849 inhibits the binding of the selective NMDA receptor antagonist, [
3
H]-(±)-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
ED
50
of 21 mg/kg.