Name | RTI-7470-44 |
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Description | RTI-7470-44 is a potent, selective human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with IC50 of 8.4 nM in vitro cAMP functional assay.RTI-7470-44 exhibits a Ki of 0.3 nM in a radioligand binding assay, and shows species selectivity (>90-fold) for hTAAR1 over the rat and mouse orthologues.RTI-7470-44 displays good blood–brain barrier permeability, moderate metabolic stability, and a favorable preliminary off-target profile.RTI-7470-44 increased the spontaneous firing rate of mouse VTA dopaminergic neurons and blocked the effects of the known TAAR1 agonist RO5166017. |
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References | 1. Ann M Decker, et al. ACS Chem Neurosci. 2022 Mar 24. doi: 10.1021/acschemneuro.2c00086. |
Molecular Formula | C19H11ClF3N5Os |
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Molecular Weight | 449.836 |