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VA012
- Soluble in DMSO
- MF: C21H19N3
- MW: 313.4
Description
VA012 is a positive allosteric modulator of the serotonin 5-HT2C receptor with an EC50 value of 16 nM. It enhances the efficacy of serotonin in a concentration-dependent manner while showing low competition with orthosteric agonists and antagonists.
VA012 is used to study allosteric enhancement of 5-HT2C receptor signaling without directly replacing endogenous serotonin. Reported profiling indicates limited off-target activity, making it useful for mechanistic studies of receptor cooperativity, serotonergic appetite pathways and biased signal amplification.
Key Features
- Potent 5-HT2C receptor PAM
- EC50: 16 nM
- Enhances serotonin efficacy dose-dependently
- Low competition with orthosteric ligands
- Limited reported off-target activity
Applications
- 5-HT2C receptor pharmacology
- Positive allosteric modulation studies
- Serotonin concentration–response assays
- Receptor-cooperativity research
- Feeding and metabolic behavior models
More Information
| Parent CAS No. | 885898-58-8 |
|---|---|
| Chemical Name | N-((1-Benzyl-1H-indol-3-yl)methyl)pyridin-3-amine |
| SMILES | C1C=C2C(CNC3C=NC=CC=3)=CN(CC3C=CC=CC=3)C2=CC=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C21H19N3/c1-2-7-17(8-3-1)15-24-16-18(20-10-4-5-11-21(20)24)13-23-19-9-6-12-22-14-19/h1-12,14,16,23H,13,15H2 |
| InChiKey | FXRHZHGEENHPFI-UHFFFAOYSA-N |
| CID | 1497577 |
| Short Description | PAM of 5-HT2C |
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