Chemical Structure : NBI-98782
CAS No.: 85081-18-1
Catalog No.: PC-49734Not For Human Use, Lab Use Only.
NBI-98782 (RRR-dihydrotetrabenazine, RRR-DHTBZ, (+)-α-HTBZ) is a potent, highly selective VMAT2 inhibitor (Ki=2 nM) and tetrabenazine metabolite.
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NBI-98782 (RRR-dihydrotetrabenazine, RRR-DHTBZ, (+)-α-HTBZ) is a potent, highly selective VMAT2 inhibitor (Ki=2 nM) and tetrabenazine metabolite.
RRR-DHTBZ displays >1000-fold selective in a broad-panel selectivity screen, including monoamine receptors.
RRR-DHTBZ displayed dose-dependent efficacy in both antipsychotic models (PPI and CAR) equivalent in magnitude to either typical or atypical antipsychotics.
RRR-DHTBZ elicited escape failures (indicative of sedation, ≥0.6 mg/kg) and at the highest dose tested produced catalepsy (motor inhibition, 1.2 mg/kg).
RRR-DHTBZ synergizes with the antipsychotics risperidone or olanzapine in suppressing conditioned avoidance behavior.
RRR-DHTBZ is effective in animal models of schizophrenia and potentiates the behavioral potency of antipsychotics in these models without potentiating weight gain.
M.Wt | 551.7 | |
Formula | C29H45NO7S | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
(2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-ol |
1. Grigoriadis DE, et al. J Pharmacol Exp Ther 361:454–461.
2. Samuel R J Hoare, et al. J Pharmacol Exp Ther. 2022 May;381(2):79-95.
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