CMPDA is a new positive allosteric modulator of AMPA. Positive allosteric modulators of AMPA receptors act by enhancing normal AMPA receptor activity to mimic long-term potentiation and prolong open-channel time by slowing or preventing channel closure. Slowing the termination of a glutamate-evoked response enhances excitatory postsynaptic potentials by increasing ion flux through AMPA receptor channels1. CMPDA modulates AMPA subunit GluA2 receptor (GluR2) and its desensitization and deactivation (EC50 values are 45.4 and 63.4 nM at GluR2i and GluR2o respectively, in a calcium influx screening assay of GluA2i and GluA2o receptors expressed in HEK293 Cell). This compound binds at the modulator binding pocket located at the interdimer interface and the clamshell hinges2. This pocket is a powerful target for drug discovery of compounds that modulate AMPA receptors and is a possible site of action for endogenous metabolites
产品描述
An AMPA Receptor Positive Allosteric Modulator
产品形式
CMPDA is a new positive allosteric modulator of AMPA. Positive allosteric modulators of AMPA receptors act by enhancing normal AMPA receptor activity to mimic long-term potentiation and prolong open-channel time by slowing or preventing channel closure. Slowing the termination of a glutamate-evoked response enhances excitatory postsynaptic potentials by increasing ion flux through AMPA receptor channels1. CMPDA modulates AMPA subunit GluA2 receptor (GluR2) and its desensitization and deactivation (EC50 values are 45.4 and 63.4 nM at GluR2i and GluR2o respectively, in a calcium influx screening assay of GluA2i and GluA2o receptors expressed in HEK293 Cell). This compound binds at the modulator binding pocket located at the interdimer interface and the clamshell hinges2. This pocket is a powerful target for drug discovery of compounds that modulate AMPA receptors and is a possible site of action for endogenous metabolites