Brain-penetrant class I ampakine with AMPA receptor (AMPAR; iGluR) positive allosteric modulator (PAM) activity both in vitro and in vivo.
CX614 (BDP-37) is a brain-penetrant class I ampakine (benzoxazine subgroup of benzamide-type) with AMPA receptor (AMPAR; iGluR) positive allosteric modulator (PAM) activity via targeting a binding site shared by cyclothiazide (CTZ), but distinct from that of GYKI 52466. CX614 enhances field excitatory postsynaptic potentials (amplitude & duration) in rat hippocampal slices and autaptically evoked excitatory postsynaptic currents in neuronal cultures (EC50 of 20-40 μM) by blocking desensitization and slowing deactivation of responses to glutamate. CX614 is also widely employed for studying AMPAR-mediated physiological responses in vivo (1-10 mg/kg n rats and mice via i.p.).
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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The Journal of neuroscience : the official journal of the Society for Neuroscience, 20(1), 8-21 (2000-01-11)
This study investigated whether positive modulators of AMPA-type glutamate receptors influence neurotrophin expression by forebrain neurons. Treatments with the ampakine CX614 markedly and reversibly increased brain-derived neurotrophic factor (BDNF) mRNA and protein levels in cultured rat entorhinal/hippocampal slices. Acute effects
The involvement of glutamate system (particularly the NMDA and AMPA receptors) in the mechanism of antidepressant activity was demonstrated in preclinical and clinical studies. In the present study, we investigated the effect of NMDA and AMPA receptors' ligands (agonists and
Journal of neurochemistry, 68(6), 2424-2434 (1997-06-01)
Homomeric AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid)-type glutamate receptors (GluRs) were stably expressed in kidney cells from cDNAs encoding GluR1 flop, GluR2 flip, GluR2 flop, and GluR3 flop subunits. The recombinant receptors were of the expected size and showed functional properties in whole-cell
Among neurobiological mechanisms underlying antidepressant properties of ketamine, structural remodeling of prefrontal and hippocampal neurons has been proposed as critical. The suggested mechanism involves downstream activation of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors, which trigger mammalian target of rapamycin (mTOR)-dependent structural plasticity
It was previously reported that Stargazin (STG) enhances the surface expression of AMPA receptors, controls receptor gating and slows channel desensitization as an auxiliary subunit of the receptors. Ampakines are a class of AMPA receptor positive allosteric modulators that modify
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