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4BP-TQS
- Soluble in DMSO
- MF: C18H17BrN2O2S
- MW: 405.31
Description
4BP-TQS is a direct allosteric agonist and positive allosteric modulator (ago-PAM) of the α7 nicotinic acetylcholine receptor (α7 nAChR). It activates α7 receptors through a transmembrane allosteric site that is topographically distinct from the orthosteric acetylcholine-binding site. In recombinant receptor studies, 4BP-TQS displayed an approximately 8-fold lower EC50 and a 45-fold larger maximal response than acetylcholine.
4BP-TQS is useful for studying receptor activation without occupancy of the classical agonist site and for dissecting the relationship between direct allosteric agonism and positive allosteric modulation. The more active (+)-enantiomer, GAT107 (Axon 2621), is also available.
Key Features
- Direct allosteric agonist and PAM of α7 nAChR (Dual-action ago-PAM)
- Selectively activates and modulates α7 nAChR
- Binds a site distinct from the acetylcholine orthosteric site
- Displays superior potency and efficacy compared to acetylcholine
Applications
- α7 nAChR allosteric activation studies
- Dual-action ago-PAM pharmacology research
- Receptor-gating and desensitization kinetics
- Stereoselective enantiomer activity profiling
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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