EPPTB Chemical Properties

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.

EPPTB Usage And Synthesis

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 +4°C

References

[1] AMYAOUCH BRADAIA. The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2009, 106 47: 20081-20086. DOI:10.1073/pnas.0906522106
[2] HENRI STALDER  Roger D N  Marius C Hoener. Selective antagonists of mouse trace amine-associated receptor 1 (mTAAR1): Discovery of EPPTB (RO5212773)[J]. Bioorganic & Medicinal Chemistry Letters, 2011, 21 4: Pages 1227-1231. DOI:10.1016/j.bmcl.2010.12.075
[3] XIAOQUN ZHANG. Striatal Tyrosine Hydroxylase Is Stimulated via TAAR1 by 3-Iodothyronamine, But Not by Tyramine or β-Phenylethylamine.[J]. Frontiers in Pharmacology, 2018: 166. DOI:10.3389/fphar.2018.00166
[4] DANILO DE GREGORIO . The hallucinogen d-lysergic diethylamide (LSD) decreases dopamine firing activity through 5-HT1A, D2 and TAAR1 receptors[J]. Pharmacological research, 2016, 113: Pages 81-91. DOI:10.1016/j.phrs.2016.08.022
[5] ELENA CICHERO. Further Insights Into the Pharmacology of the Human Trace Amine-Associated Receptors: Discovery of Novel Ligands for TAAR1 by a Virtual Screening Approach[J]. Chemical Biology & Drug Design, 2014, 84 6: 712-720. DOI:10.1111/cbdd.12367
[6] XUEHONG LIU A J David K Grandy. Ractopamine, a livestock feed additive, is a full agonist at trace amine-associated receptor 1.[J]. Journal of Pharmacology and Experimental Therapeutics, 2014, 350 1: 124-129. DOI:10.1124/jpet.114.213116

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