ampa receptor desensitization

Cyclothiazide is a benzothiadiazide that acts as a potentiator of AMPA receptorsthat potently inhibits AMPA receptor desensitization, positively modulating its response to glutamic acid (EC50 = 3.8 M).

TDPAM02 is a positive allosteric modulator of the AMPA receptor GluA2. It specifically binds to the ligand-binding domain (LBD) of GluA2, with an IC50 of 1.4 nM for the GluA2 flop isoform. TDPAM02 stabilizes the activated conformation of the GluA2 receptor, delaying receptor inactivation or desensitization and maintaining rapid excitatory synaptic transmission in the central nervous system.

TDPAM01 acts as a positive allosteric modulator of the AMPA receptor GluA2. It specifically binds to the ligand-binding domain (LBD) of GluA2, with an IC50 value of 13.4 nM for the GluA2 flop subtype. TDPAM01 stabilizes the active conformation of the GluA2 receptor, delaying receptor inactivation or desensitization, thereby sustaining rapid excitatory synaptic transmission in the central nervous system.

JAMI1001A is a positive allosteric modulator of the AMPA receptor, effectively modulating the deactivation and desensitization of both [flip] and [flop] receptor isoforms.

AMPA receptor modulator-6 is a unique dimeric positive allosteric modulator that effectively stabilizes the dimer interface of AMPA receptors by physically bridging two adjacent ligand-binding domains. This structural anchoring significantly slows receptor desensitization and deactivation, thereby enhancing glutamate-mediated synaptic transmission.