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EPPTB
- RO 5212773
Axon 2419
CAS:
1110781-88-8
Purity:
100%
- Soluble in DMSO
- MF: C20H21F3N2O2
- MW: 378.39
Description
The first, highly potent and selective full antagonist of the trace amine-associated receptor 1 (TAAR1; IC50 value 28 nM at mouse TAAR1). EPPTB blocks the TAAR1-mediated activation of an inwardly rectifying K+ channels.
A useful pharmacological tool for in vitro and in vivo investigations to study the role of TAAR1 in psychiatric and neurodegenerative disorders.
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 |
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.
