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4BP-TQS
- Soluble in DMSO
- MF: C18H17BrN2O2S
- MW: 405.31
Description
4BP-TQS is an allosteric agonist of α7 nicotinic acetylcholine receptors (nAChR). The agonism was shown to act through a site topographically distinct from the ACh site. 4BP-TQS was a more potent and efficacious agonist of α7 nAChR than ACh (8-fold lower EC50 and 45-fold larger maximal response).
The bioactive enantiomer of 4BP-TQS, GAT107 (Axon 2621), is also available.
More Information
| Parent CAS No. | 360791-49-7 |
|---|---|
| Chemical Name | 4-(4-Bromophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide |
| SMILES | C1C(S(N)(=O)=O)=CC2C3C=CCC3C(C3C=CC(Br)=CC=3)NC=2C=1 |
| MFCD | MFCD00981752 |
| InChi | InChI=1S/C18H17BrN2O2S/c19-12-6-4-11(5-7-12)18-15-3-1-2-14(15)16-10-13(24(20,22)23)8-9-17(16)21-18/h1-2,4-10,14-15,18,21H,3H2,(H2,20,22,23) |
| InChiKey | YNCXHXYZTLIZTO-UHFFFAOYSA-N |
| CID | 2857838 |
| Short Description | α7 nAChR allosteric agonist |
References
- JK Gill et al. Agonist activation of alpha7 nicotinic acetylcholine receptors via an allosteric transmembrane site. Proc Natl Acad Sci USA. 2011 Apr 5;108(14):5867-72.
- RL Papke. The activity of GAT107, an allosteric activator and positive modulator of α7 nicotinic acetylcholine receptors (nAChR), is regulated by aromatic amino acids that span the subunit interface. J Biol Chem. 2014 Feb 14;289(7):4515-31.
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