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.
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
