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Chemical Structure : EPPTB
Catalog No.: PC-61073Not For Human Use, Lab Use Only.
EPPTB (RO5212773) is a potent, selective mouse TAAR1 antagonist that potently antagonizes cAMP production induced by 1.5 uM β-phenylethylamine with IC50 of 27.5 nM, Ki of 1 nM.
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EPPTB (RO5212773) is a potent, selective mouse TAAR1 antagonist that potently antagonizes cAMP production induced by 1.5 uM β-phenylethylamine with IC50 of 27.5 nM, Ki of 1 nM; displays >1,000-fold selectivity over dopamine, serotonin and adrenergic receptors; dose-dependently reduces cAMP levels in HEK293 cells in the absence of TAAR1 agonist with IC50 of 19±12 nM, significantly more potent in antagonizing cAMP production by mouse, as compared to rat and human; blocks the TAAR1-mediated activation of an inwardly rectifying K(+) current at dopamine (DA) neurons of the ventral tegmental area.
| M.Wt | 378.395 | |
| Formula | C20H21F3N2O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Bradaia A, et al. Proc Natl Acad Sci U S A. 2009 Nov 24;106(47):20081-6.
2. Stalder H, et al. Bioorg Med Chem Lett. 2011 Feb 15;21(4):1227-31.
3. Leo D, et al. Neuropharmacology. 2014 Jun;81:283-91.
4. Liu X, et al. J Pharmacol Exp Ther. 2014 Jul;350(1):124-9.
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