Anticonvulsant action and biochemical effects in DBA/2 mice of CPP (3-((±)-2-carboxypiperazin-4-yl)-propyl-1-phosphonate), a novel N-methyl-D-aspartate antagonist

Chapman, A. Chaston; Meldrun, Brian S.; Nanji, N.; Watkins, Johnathan

doi:10.1016/0014-2999(87)90501-2

Cited by 54 publications

(5 citation statements)

References 12 publications

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“…Both intraperitoneal injection and intracortical infusion of the selective NMDA receptor antagonist CPP raised extracellular GLU in the mPFC of awake rats and the blockade of 5‐HT 2A receptors prevented the effect of locally infused CPP. The systemic dose and the intracortical concentration of CPP that significantly increased extracellular GLU fit well with those used in vitro and in vivo to selectively block NMDA receptors (Chapman et al. 1987; Lehmann et al.…”

Section: Discussionsupporting

confidence: 55%

“…GLU in the mPFC of awake rats and the blockade of 5-HT 2A receptors prevented the effect of locally infused CPP. The systemic dose and the intracortical concentration of CPP that significantly increased extracellular GLU fit well with those used in vitro and in vivo to selectively block NMDA receptors (Chapman et al 1987;Lehmann et al 1987;Del Arco and Mora 2002). In addition, intracortical infusion of the competitive NMDA receptors antagonist AP7 (Perkins et al 1982) also raised extracellular GLU (see Results).…”

Section: -Ht 2a Receptors and Extracellular Glu 193supporting

confidence: 58%

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The 5‐HT_2A receptor antagonist M100,907 prevents extracellular glutamate rising in response to NMDA receptor blockade in the mPFC

Ceglia

Carli

Baviera

et al. 2004

Journal of Neurochemistry

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We recently found that intracortical injection of the selective and competitive N-methyl-D-aspartate (NMDA) receptor antagonist 3-(R)-2-carboxypiperazin-4-propyl-1-phosphonic acid (CPP) impaired attentional performance in rats and blockade of 5-hydroxytryptamine (5-HT) 2A receptors antagonized this effect. Here, we used the microdialysis technique in conscious rats to study the effect of CPP on extracellular glutamate (GLU) in the medial prefrontal cortex (mPFC) and the regulation of this effect by 5-HT 2A receptors. Intraperitoneal injection of 20 mg/kg CPP increased extracellular GLU in the mPFC (201% of basal levels) but had no effect on 5-HT. Intracortical infusion of 100 lM CPP increased extracellular GLU (230% of basal values) and 5-HT (150% of basal values) in the mPFC, whereas 30 lM had no significant effect. The effect of 100 lM CPP on extracellular GLU was abolished by tetrodotoxin, suggesting that neuronal activity is required. Subcutaneous injection of 40 lg/kg M100,907 completely antagonized the effect of 100 lM CPP on extracellular GLU, whereas 10 lg/kg caused only partial attenuation. Likewise, intracortical infusion of 0.1 lM M100,907 completely reversed the increase of extracellular GLU induced by CPP. These findings show that blockade of NMDA receptors in the mPFC is sufficient to increase extracellular GLU locally. The increase of cortical extracellular GLU may contribute to CPP-induced cognitive deficits and blockade of 5-HT 2A receptors may provide a molecular mechanism for reversing these deficits caused by dysfunctional glutamatergic transmission in the mPFC.

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Section: Discussionsupporting

confidence: 55%

Section: -Ht 2a Receptors and Extracellular Glu 193supporting

confidence: 58%

The 5‐HT_2A receptor antagonist M100,907 prevents extracellular glutamate rising in response to NMDA receptor blockade in the mPFC

Ceglia

Carli

Baviera

et al. 2004

Journal of Neurochemistry

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“…Chapman et al (1987) showed that injection of 3-[(+/ -)-2-carboxypiperazin-4-yl] propyl-l-phosphonate (CPP), a non-competitive antagonist of NMDA receptors, inhibited convulsion of audiogenic DBA/2 mice. They found that the anticonvulsant action of CPP was much stronger than that of AP7, a competitive antagonist of NMDA receptors.…”

Section: Discussionmentioning

confidence: 99%

Spider toxin (JSTX-3) inhibits the convulsions induced by glutamate agonists

Himi

Saito

Kawai

et al. 1990

J. Neural Transmission

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The effect of a spider toxin (JSTX-3)--a specific blocker of glutamate receptors--on the behavior of mice was studied using an intracerebroventricular (i.c.v.) injection technique. At higher doses (more than 12 nmol/brain), JSTX-3 increased motor activities and induced characteristic symptoms. JSTX-3 at a dose of 4.7 nmol/brain which per se did not produce any abnormal behavior, specifically antagonized quisqualate-induced convulsions but not NMDA- or kainate-induced convulsions. These results indicate that JSTX-3 is a selective antagonist of the quisqualate receptors in the mammalian central nervous system.

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“…Anticonvulsant activity was evaluated in groups of male mice (CD1 Charles River) against tonic convulsions induced by supramaximal electroshock, according to the method described by Swinyard et al [1952], or against audiogenic seizures in 21-day-old DBA2 mice [Chapman et al, 1987]. For supramaximal electroshock, 1 was administered to groups of six male mice (bw 18-22 g) at 20, 40, 80, and 160 mg/kg ip in 1% Tween, with a control group receiving vehicle alone.…”

Section: Anticonvulsant Activitymentioning

confidence: 99%

Synthesis and pharmacological properties of 5H,10H-imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one, a new competitive AMPA/KA receptor antagonist

et al. 1999

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Anticonvulsant action and biochemical effects in DBA/2 mice of CPP (3-((±)-2-carboxypiperazin-4-yl)-propyl-1-phosphonate), a novel N-methyl-D-aspartate antagonist

Cited by 54 publications

References 12 publications

The 5‐HT_2A receptor antagonist M100,907 prevents extracellular glutamate rising in response to NMDA receptor blockade in the mPFC

The 5‐HT_2A receptor antagonist M100,907 prevents extracellular glutamate rising in response to NMDA receptor blockade in the mPFC

Spider toxin (JSTX-3) inhibits the convulsions induced by glutamate agonists

Synthesis and pharmacological properties of 5H,10H-imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one, a new competitive AMPA/KA receptor antagonist

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Anticonvulsant action and biochemical effects in DBA/2 mice of CPP (3-((±)-2-carboxypiperazin-4-yl)-propyl-1-phosphonate), a novel N-methyl-D-aspartate antagonist

Cited by 54 publications

References 12 publications

The 5‐HT2A receptor antagonist M100,907 prevents extracellular glutamate rising in response to NMDA receptor blockade in the mPFC

The 5‐HT2A receptor antagonist M100,907 prevents extracellular glutamate rising in response to NMDA receptor blockade in the mPFC

Spider toxin (JSTX-3) inhibits the convulsions induced by glutamate agonists

Synthesis and pharmacological properties of 5H,10H-imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one, a new competitive AMPA/KA receptor antagonist

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The 5‐HT_2A receptor antagonist M100,907 prevents extracellular glutamate rising in response to NMDA receptor blockade in the mPFC

The 5‐HT_2A receptor antagonist M100,907 prevents extracellular glutamate rising in response to NMDA receptor blockade in the mPFC