Identification | Back Directory | [Name]
EPPTB | [CAS]
1110781-88-8 | [Synonyms]
EPPTB RO5212773) EPPTB
(RO 5212773 Ro 5212773 (EPPTB) N-(3-Ethoxy-phenyl)-4-pyrrolidin-1-yl-3-trifluoromethyl-benzamide N-(3-Ethoxyphenyl)-4-(1-pyrrolidinyl)-3-(trifluoromethyl)benzamide Benzamide, N-(3-ethoxyphenyl)-4-(1-pyrrolidinyl)-3-(trifluoromethyl)- | [Molecular Formula]
C20H21F3N2O2 | [MDL Number]
MFCD21605509 | [MOL File]
1110781-88-8.mol | [Molecular Weight]
378.39 |
Chemical Properties | Back Directory | [storage temp. ]
-20°C | [solubility ]
Soluble in DMSO (up to 25 mg/ml). | [form ]
solid | [color ]
White | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
Hazard Information | Back Directory | [Description]
EPPTB (1110781-88-8) is a novel selective trace amine associated receptor 1 (TAAR1) antagonist (IC50=28 nM at mouse TAAR1).1,2 A useful tool for probing the physiologic role of TAAR1.3-6 | [Uses]
EPPTB is a selective antagonist of the trace amine-associated 1 (TA1) receptor, increasing the firing frequency of dopamine (DA) neurons in the ventral tegmental area. This makes it a promising drug target for neurodegenerative disorders. | [storage]
Store at -20°C | [References]
1) Bradaia et al. (2009), The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system; Proc. Natl. Acad. Sci. USA, 106 20081
2) Stalder et al. (2011), Selective antagonists of mouse trace amine-associated receptor 1 (mTAAR1): discovery of EPPTB (RO5212773); Bioorg. Med. Chem. Lett., 21 1227
3) Zhang et al. (2018), Striatal Tyrosine Is Stimulated via TAAR1 by 3-Iodothyronamine, But Not by Tyramine or β-Phenylethylamine; Front. Pharmacol., 9 166
4) De Greggrio et al. (2016), The hallucinogen d-lysergic diethylamide (LSD) decreases dopamine firing activity through 5-HT1A, D2 and TAAR1 receptors; Pharmacol. Res., 113 81
5) Cichero et al. (2014), Further insights into the pharmacology of the human trace amine-associated receptors: discovery of the novel ligands for TAAR1 by a virtual screening approach; Chem. Biol. Drug Des., 84 712
6) Liu et al. (2014), Ractopamine, a livestock feed additive, is a full agonist at trace amine-associated receptor 1; J. Pharmacol. Exp. Ther. 350 124 |
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