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EPPTB
- RO 5212773
Axon 2419
CAS:
1110781-88-8
Purity:
100%
- Soluble in DMSO
- MF: C20H21F3N2O2
- MW: 378.39
Description
EPPTB (RO 5212773) is a potent antagonist of trace amine-associated receptor 1 (TAAR1), originally characterized at mouse TAAR1. It blocks TAAR1-mediated signaling and downstream modulation of inwardly rectifying potassium channels.
TAAR1 is a monoaminergic GPCR involved in trace amine, dopamine and psychostimulant-related signaling. EPPTB provides a pharmacological antagonist for investigating TAAR1 function in neuropsychiatric, dopaminergic and monoamine-regulated systems.
Key Features
- Potent TAAR1 antagonist
- Reported IC50: 28 nM at mouse TAAR1
- Blocks TAAR1-mediated activation of inwardly rectifying K+ channels
- Useful tool for trace-amine and monoamine receptor pharmacology
Applications
- TAAR1 receptor pharmacology
- Dopamine and trace-amine signaling studies
- Neuropsychiatric pathway research
- GPCR antagonist assay development
More Information
| Parent CAS No. | 1110781-88-8 |
|---|---|
| Chemical Name | N-(3-ethoxyphenyl)-4-(pyrrolidin-1-yl)-3-(trifluoromethyl)benzamide |
| SMILES | C1(C(F)(F)F)C=C(C(NC2C=CC=C(OCC)C=2)=O)C=CC=1N1CCCC1 |
| MFCD | MFCD21605509 |
| InChi | InChI=1S/C20H21F3N2O2/c1-2-27-16-7-5-6-15(13-16)24-19(26)14-8-9-18(25-10-3-4-11-25)17(12-14)20(21,22)23/h5-9,12-13H,2-4,10-11H2,1H3,(H,24,26) |
| InChiKey | KLFVWQCQUXXLOU-UHFFFAOYSA-N |
| CID | 25175634 |
| Short Description | TAAR1 antagonist |
EPPTB (RO 5212773)
potent TAAR1 antagonist
EPPTB
RO 5212773
MFCD21605509
RO5212773
TAAR1
DRD2
D2
trace amine associated receptor
dopamine
DA
Antagonist
GPCR signaling
dopamine signaling
TAAR1 receptor pharmacology
Dopamine and trace-amine signaling studies
Neuropsychiatric pathway research
GPCR antagonist assay development
GPCR pharmacology
signal transduction
receptor pharmacology
neuroscience
GPCR
CAS 1110781-88-8
Axon Medchem
Axon 2419
Supplier
Vendor
References
- H. Stalder et al. Selective antagonists of mouse trace amine-associated receptor 1 (mTAAR1): discovery of EPPTB (RO5212773). Bioorg Med Chem Lett. 2011 Feb 15;21(4):1227-31.
- A. Bradaia et al. The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system. Proc Natl Acad Sci U S A. 2009 Nov 24;106(47):20081-6.
