1204572-55-3

BPAM344 is a kainate receptor (KAR) subunits GluK1b, GluK2a, and GluK3a positive allosteric modulator (PAM)[1].

BPAM344 is a kainate receptor (KAR) subunits GluK1b, GluK2a, and GluK3a positive allosteric modulator (PAM)[1]. BPAM344 potentiates glutamate-evoked currents of GluK2a 21-fold at the highest concentration tested (200 μM), with an EC50 of 79 μM. BPAM344 markedly decreases desensitization kinetics (from 5.5 to 775 ms), whereas it only has a minor effect on deactivation kinetics[1]. BPAM344 (100 μM) also potentiates the peak current amplitude of KAR subunits GluK3a (59-fold), GluK2a (15-fold), GluK1b (5-fold), as well as the AMPA receptor subunit GluA1i (5-fold)[1].

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[1]. Anja Probst Larsen, et al. Identification and Structure-Function Study of Positive Allosteric Modulators of Kainate Receptors. Mol Pharmacol. 2017 Jun;91(6):576-585.