2231101-34-9
Chemical Structure
TDPAM02
- CAS No.: 2231101-34-9
- Formula:C22H26N4O4S2
- Molecular Weight:474.59
IUPAC Name: 6,6'-(ethane-1,2-diyl)bis(4-cyclopropyl-3,4-dihydro-2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide)
InChIKey: TVWVZMLPANTKEA-UHFFFAOYSA-N
SMILES: O=S1(=O)NCN(C2=CC(=CC=C21)CCC3=CC=C4C(=C3)N(CNS4(=O)=O)C5CC5)C6CC6
Biological Activity: TDPAM02 is a potent positive allosteric modulator of the AMPA receptor GluA2 subunit, with an EC50 of 1.4 nM for the GluA2 flop (Q) subunit. TDPAM02 binds at the dimer interface of the GluA2 ligand-binding domain and stabilizes the receptor conformation by simultaneously occupying two allosteric sites, thereby significantly slowing the receptor desensitization process and maintaining rapid excitatory synaptic transmission in the central nervous system. TDPAM02 is also a positive allosteric modulator of the GluK1 receptor. TDPAM02 can be used for research on neurological diseases[1][2][3].
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TDPAM02 | TDPAM02 is a potent positive allosteric modulator of the AMPA receptor GluA2 subunit, with an EC50 of 1.4 nM for the GluA2 flop (Q) subunit. TDPAM02 binds at the dimer interface of the GluA2 ligand-binding domain and stabilizes the receptor conformation by simultaneously occupying two allosteric sites, thereby significantly slowing the receptor desensitization process and maintaining rapid excitatory synaptic transmission in the central nervous system. TDPAM02 is also a positive allosteric modulator of the GluK1 receptor. TDPAM02 can be used for research on neurological diseases. | |||||||||||||||||||||
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References
- [1]. Laulumaa S, et al. Crystal Structures of Potent Dimeric Positive Allosteric Modulators at the Ligand-Binding Domain of the GluA2 Receptor. ACS medicinal chemistry letters. 2019 Mar 14;10(3):243-247. [Content Brief]
- [2]. Zhigulin AS, et al. The diversity of AMPA receptor inhibition mechanisms among amidine-containing compounds. Frontiers in pharmacology. 2024;15:1467266. [Content Brief]
- [3]. Bay Y, et al. Crystal structure of the GluK1 ligand-binding domain with kainate and the full-spanning positive allosteric modulator BPAM538. Journal of structural biology. 2024 Sep;216(3):108113. [Content Brief]
