1110781-88-8

1110781-88-8 structure

Name: EPPTB
Chemical Name: N-(3-ethoxy-phenyl)-4-pyrrolidin-1-yl-3-trifluoromethylbenzamide
CAS Number: 1110781-88-8
Molecular Formula: C₂₀H₂₁F₃N₂O₂
Molecular Weight: 378.39
Catalog: Research Areas Neurological Disease
Create Date: 2018-04-23 16:28:21
Modify Date: 2024-01-06 11:06:07
Ro 5212773 (EPPTB) is a potent and selective trace amine-associated receptor 1 (TAAR1) antagonist (Ki=0.9 nM for mouse TAAR1), with no significant effects on other TAARs. TAAR1 is a G protein-coupled receptor (GPCR) that is nonselectively activated by endogenous metabolites of amino acids[1][2].

Name	N-(3-ethoxy-phenyl)-4-pyrrolidin-1-yl-3-trifluoromethylbenzamide
Synonyms	EPPTB RO5212773 N-(3-ethoxy-phenyl)-4-pyrrolidin-1-yl-3-trifluoromethyl-benzamide BENZAMIDE, N-(3-ETHOXYPHENYL)-4-(1-PYRROLIDINYL)-3-(TRIFLUOROMETHYL)-

Description	Ro 5212773 (EPPTB) is a potent and selective trace amine-associated receptor 1 (TAAR1) antagonist (Ki=0.9 nM for mouse TAAR1), with no significant effects on other TAARs. TAAR1 is a G protein-coupled receptor (GPCR) that is nonselectively activated by endogenous metabolites of amino acids[1][2].
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Neurological Disease
In Vitro	Ro 5212773 (EPPTB) suppresses the excitability of hippocampal pyramidal neurons. EPPTB also reduceds seizure-like events (SLEs) and seizure activity[1]. Ro 5212773 blocks the TAAR1-mediated activation of an inwardly rectifying K+ current[2]. Ro 5212773 potently antagonizes cAMP production induced by activating mouse TAAR1 with 1.5 μM β-phenylethylamine (IC50=27.5 nM). cAMP levels are dose-dependently reduced by Ro 5212773 in HEK293 cells in the absence of TAAR1 agonist (IC50= 19 nM). EPPTB is significantly more potent in antagonizing cAMP production by mouse, as compared to rat (IC50= 4539 nM) and human (IC50= 7487 nM) TAAR1[2].
References	[1]. Bradaia A, 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;106(47):20081-20086.

RIDADR	NONH for all modes of transport