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NBI-98782

Chemical Structure : NBI-98782

CAS No.: 85081-18-1

NBI-98782 (NBI 98782, RRR-DHTBZ, (+)-α-HTBZ)

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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 551.7
Formula C29H45NO7S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

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

References

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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