Trace amine 1 (TA1) receptor antagonist/inverse agonist; exhibits a higher potency at the mouse TA1 receptor than the rat and human TA1 receptors (IC50 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 (IC50 = 19 nM).
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 378.39. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.64 mL||13.21 mL||26.43 mL|
|5 mM||0.53 mL||2.64 mL||5.29 mL|
|10 mM||0.26 mL||1.32 mL||2.64 mL|
|50 mM||0.05 mL||0.26 mL||0.53 mL|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
References are publications that support the products' biological activity.
Bradaia et al (2009) The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system. Proc.Natl.Acad.Sci.U.S.A. 106 20081 PMID: 19892733
If you know of a relevant reference for EPPTB, please let us know.
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Keywords: Parkinson's disease trace amine-associated receptors 1 TAAR1 antagonists dopamine neurons neurones TA1 Trace Amine 1 Receptor
Citations for EPPTB
Citations are publications that use Tocris products.
Currently there are no citations for EPPTB. Do you know of a great paper that uses EPPTB from Tocris? If so please let us know.
Literature in this Area
Dopamine Receptors Scientific Review
Written by Phillip Strange and revised by Kim Neve in 2013, this review summarizes the history of the dopamine receptors and provides an overview of individual receptor subtype properties, their distribution and identifies ligands which act at each receptor subtype. Compounds available from Tocris are listed.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.