EPPTB (RO-5212773) is a drug developed by
Hoffmann-La Roche which acts as a potent and selective
inverse agonist of
trace amine-associated receptor 1 (TAAR1), with no significant activity at other targets. EPPTB is one of the first selective antagonists developed for TAAR1, and has been used to demonstrate an important role for TAAR1 in regulation of
dopaminergic signalling in the
limbic system.[1] Although EPPTB has high affinity for the mouse TAAR1, it has much lower affinity for rat and human TAAR1, which limits its use in research.[2] While the human and mouse forms of TAAR1 have similar functions and bind similar ligands, the actual binding affinities of individual ligands often vary significantly between the two versions of the receptor.[3]
^Hu LA, Zhou T, Ahn J, Wang S, Zhou J, Hu Y, Liu Q (October 2009). "Human and mouse trace amine-associated receptor 1 have distinct pharmacology towards endogenous monoamines and imidazoline receptor ligands". The Biochemical Journal. 424 (1): 39–45.
doi:
10.1042/BJ20090998.
PMID19725810.
S2CID21498991.
† References for all endogenous human TAAR1 ligands are provided at
List of trace amines
‡ References for synthetic TAAR1 agonists can be found at
TAAR1 or in the associated compound articles. For TAAR2 and TAAR5 agonists and inverse agonists, see
TAAR for references.