Trace amine 1 (TA1
) receptor antagonist/inverse agonist; exhibits a higher potency at the mouse TA1
receptor than the rat and human TA1
values are 27.5, 4539 and 7487 nM, respectively). Blocks the TA1
receptor-mediated activation of an inwardly rectifying K+
current, which increases the firing frequency of dopamine (DA) neurons in the ventral tegmental area. Increases DA potency at the D2
receptor. Also displays inverse agonism, reducing basal cAMP levels in vitro
= 19 nM).
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The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system.
Bradaia et al.