EPPTB

EPPTB
Clinical data
Other names	Ro 5212773; Ro-5212773; Ro5212773; RO-5212773; RO5212773
Drug class	Trace amine-associated receptor 1 (TAAR1) antagonist or inverse agonist
Identifiers
	IUPAC name N-(3-ethoxyphenyl)-4-pyrrolidin-1-yl-3-trifluoromethylbenzamide;
CAS Number	1110781-88-8;
PubChem CID	25175634;
IUPHAR/BPS	5457;
ChemSpider	26387935;
ChEMBL	ChEMBL1669669;
CompTox Dashboard (EPA)	DTXSID501030324 ;
Chemical and physical data
Formula	C20H21F3N2O2
Molar mass	378.395 g·mol−1
3D model (JSmol)	Interactive image; Interactive image;
	SMILES CCOc2cc(ccc2)NC(=O)c(cc1C(F)(F)F)ccc1N3CCCC3; ; CCOc1cccc(c1)NC(=O)c2ccc(c(c2)C(F)(F)F)N3CCCC3;
	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); Key:KLFVWQCQUXXLOU-UHFFFAOYSA-N;

EPPTB, also known as RO5212773 or RO-5212773, is a drug developed by Hoffmann-La Roche which acts as a potent and selective antagonist or inverse agonist of the trace amine-associated receptor 1 (TAAR1).^[1]^[2]^[3]^[4] The drug was the first selective antagonist developed for the TAAR1.^[2]^[3] It is a potent agonist of the mouse and rat TAAR1, but is dramatically less potent as an agonist of the human TAAR1.^[5]^[2]^[3] EPPTB has been used in scientific research to demonstrate an important role for TAAR1 in regulation of dopaminergic signaling in the limbic system.^[2]^[3]

^ Cite error: The named reference LiuLi2018 was invoked but never defined (see the help page).
^ ^a ^b ^c ^d Bradaia A, Trube G, Stalder H, Norcross RD, Ozmen L, Wettstein JG, et al. (November 2009). "The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system". Proceedings of the National Academy of Sciences of the United States of America. 106 (47): 20081–20086. Bibcode:2009PNAS..10620081B. doi:10.1073/pnas.0906522106. PMC 2785295. PMID 19892733.
^ ^a ^b ^c ^d Cite error: The named reference StalderHoenerNorcross2011 was invoked but never defined (see the help page).
^ Gainetdinov RR, Hoener MC, Berry MD (July 2018). "Trace Amines and Their Receptors". Pharmacol Rev. 70 (3): 549–620. doi:10.1124/pr.117.015305. PMID 29941461.
^ Cite error: The named reference DeckerBrackeenMohammadkhani2022 was invoked but never defined (see the help page).

[LiuLi2018-1] Cite error: The named reference LiuLi2018 was invoked but never defined (see the help page).

[BradaiaTrubeStalder2009-2] Bradaia A, Trube G, Stalder H, Norcross RD, Ozmen L, Wettstein JG, et al. (November 2009). "The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system". Proceedings of the National Academy of Sciences of the United States of America. 106 (47): 20081–20086. Bibcode:2009PNAS..10620081B. doi:10.1073/pnas.0906522106. PMC 2785295. PMID 19892733.

[StalderHoenerNorcross2011-3] Cite error: The named reference StalderHoenerNorcross2011 was invoked but never defined (see the help page).

[GainetdinovHoenerBerry2018-4] Gainetdinov RR, Hoener MC, Berry MD (July 2018). "Trace Amines and Their Receptors". Pharmacol Rev. 70 (3): 549–620. doi:10.1124/pr.117.015305. PMID 29941461.

[DeckerBrackeenMohammadkhani2022-5] Cite error: The named reference DeckerBrackeenMohammadkhani2022 was invoked but never defined (see the help page).

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