PEAQX is a potent and orally active NMDA antagonist with a 15-fold preference for human NMDA receptors with the 1A/2A (IC50=270 nM), rather than 1A/2B(29,600 nM).
PEAQX 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Mouse cortical neurons
400 nM
20 minutes
To evaluate the effect of NMDA-R antagonists on neuronal excitotoxicity. Ro25-6981 (NR2B antagonist) reversed NMDA-induced excitotoxicity, while NVP-AAM077 (NR2A antagonist) had no significant effect.
PEAQX failed to significantly affect the APV-sensitive tonic I NMDA and its variance. In PEAQX preincubated slices, 24HC still significantly increased the APV-sensitive tonic I NMDA and its variance.
Neuropharmacology. 2019 Apr;148:11-20.
Corticostriatal organotypic slice cultures
3 µM
12 hours
PEAQX dose-dependently activates caspase-3, while ifenprodil shows no effect.
Neuroscience. 2009 Nov 10;163(4):1181-91.
PEAQX 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Rats
Freely moving rats
Intraperitoneal injection
10 mg/kg
Single injection, at least 4 days apart
Tested the effect of PEAQX on cortical gamma oscillations, results showed 10 mg/kg PEAQX was ineffective
Biol Psychiatry. 2012 Jun 1;71(11):987-95
Rats
Cocaine self-administration and extinction training model
Bilateral intra-DH microinfusions
2.5 μg per 0.5 μl per hemisphere
Single administration
To evaluate the effects of PEAQX on cocaine-memory reconsolidation, results showed that PEAQX attenuated subsequent drug context-induced cocaine-seeking behavior
Neuropsychopharmacology. 2016 Feb;41(3):675-85
Rats
Developing rats
Subcutaneous injection
5, 10, 20 mg/kg
Single administration
To evaluate the anticonvulsant effects of PEAQX in rats of different age groups. Results showed that PEAQX exhibited anticonvulsant activity in all age groups tested, but its effects varied qualitatively and quantitatively depending on the age of animals, dose, and seizure model.
Pharmaceutics. 2021 Mar 19;13(3):415
Sprague-Dawley rats
Pups
Subcutaneous injection
10, 20 or 40 mg/kg
Once on PN7, 9, and 11
PEAQX resulted in caspase-3 activation in the frontal cortex and striatum 8 hrs after the last of 3 injections.
Neuroscience. 2009 Nov 10;163(4):1181-91.
Mice
MAO A KO mice
Intraperitoneal injection
2 mg/kg
Single dose
To evaluate the effect of PEAQX on aggressive behavior in MAO A KO mice, results showed PEAQX significantly reduced aggressive behavior
J Neurosci. 2012 Jun 20;32(25):8574-82
Mice
Chronic ethanol exposure model
Intraperitoneal injection
10 μM
Once daily for 28 days
To investigate the effect of chronic ethanol exposure on facial stimulation-evoked MF-GC synaptic transmission in the mouse cerebellar cortex, and found that PEAQX (10 μM) abolished this enhancement.
Front Syst Neurosci. 2021 Aug 2;15:657884
Male Sprague-Dawley rats
Social interaction test
Subcutaneous injection
2.5, 5, 10, 20 mg/kg
Single administration, 10 min prior
To assess the inhibitory effects of PEAQX on social behavior in adolescent and adult rats. Adolescents showed social inhibition at doses of 10 and 20 mg/kg, whereas adults only showed this effect at 20 mg/kg.
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