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Chemical Structure : BRD5814
Catalog No.: PC-63349Not For Human Use, Lab Use Only.
BRD5814 is a potent, selective, highly brain penetrant β-arrestin biased dopamine D2 receptor (D2R) antagonist with Ki of 0.27 uM.
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BRD5814 is a potent, selective, highly brain penetrant β-arrestin biased dopamine D2 receptor (D2R) antagonist with Ki of 0.27 uM.
BRD5814 strongly diminish D2R/β-arrestin signaling (EC50=0.54 uM) without affecting D2R/Gαi signaling.
BRD5814 demonstrates good target engagement via PET imaging, achieving efficacy in an amphetamine-induced hyperlocomotion mouse model with strongly reduced motoric side effects in a rotarod performance test.
| M.Wt | 413.865 | |
| Formula | C21H23ClF3NO2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Weïwer M, et al. ACS Chem Biol. 2018 Apr 20;13(4):1038-1047.
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