SML2047
BPAM344
≥98% (HPLC)
Synonym(s):
BPAM344, 4-Cyclopropyl-3,4-dihydro-7-fluoro-2H-1,2,4-benzothiadiazine 1,1-dioxide
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assay
≥98% (HPLC)
form
powder
color
white to beige
storage temp.
2-8°C
SMILES string
O=S1(C2=CC(F)=CC=C2N(C3CC3)CN1)=O
Biochem/physiol Actions
BPAM344 is a potent positive allosteric modulator (PAM) on the three KAR subunits GluK1b, GluK2a, and GluK3a. BPAM344 potentiates glutamate-evoked currents of GluK2a 21-fold, and noticeably decreases desensitization kinetics (from 5.5 to 775 ms).
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Biophysical journal, 110(11), 2397-2406 (2016-06-09)
The 1,2,4-benzothiadiazine 1,1-dioxide type of positive allosteric modulators of the ionotropic glutamate receptor A2 (GluA2) are promising lead compounds for the treatment of cognitive disorders, e.g., Alzheimer's disease. The modulators bind in a cleft formed by the interface of two
Molecular pharmacology, 91(6), 576-585 (2017-04-01)
Kainate receptors (KARs) consist of a class of ionotropic glutamate receptors, which exert diverse pre- and postsynaptic functions through complex signaling regulating the activity of neural circuits. Whereas numerous small-molecule positive allosteric modulators of the ligand-binding domain of (
Journal of medicinal chemistry, 56(21), 8736-8745 (2013-10-18)
Positive allosteric modulators of ionotropic glutamate receptors are potential compounds for treatment of cognitive disorders, e.g., Alzheimer's disease. The modulators bind within the dimer interface of the ligand-binding domain (LBD) and stabilize the agonist-bound conformation, thereby slowing receptor desensitization and/or
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