An inhibitor of VMAT2 and an active metabolite of tetrabenazine and valbenazine
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NBI 98782

Item No. 42116

Product Insert (PDF)
Technical Information
Formal Name
(2R)-1,3R,4,6,7,11bR-hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-2H-benzo[a]quinolizin-2-ol
CAS Number
85081-18-1
Synonyms
  • α-Dihydrotetrabenazine
  • α-DTBZ
Molecular Formula
C19H29NO3
Formula Weight
Purity
≥98%
A solid
DMSO: Sparingly Soluble: 1-10 mg/mlEthanol: Sparingly Soluble: 1-10 mg/ml
SMILES
COC1=C(OC)C=C2CCN(C[C@H]([C@@H](C3)O)CC(C)C)[C@@]3([H])C2=C1
InChi Code
InChI=1S/C19H29NO3/c1-12(2)7-14-11-20-6-5-13-8-18(22-3)19(23-4)9-15(13)16(20)10-17(14)21/h8-9,12,14,16-17,21H,5-7,10-11H2,1-4H3/t14-,16-,17-/m1/s1
InChi Key
WEQLWGNDNRARGE-DJIMGWMZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    NBI 98782 is an inhibitor of vesicular monoamine transport 2 (VMAT2; Ki = 3.96 nM) and an active metabolite of tetrabenazine (Item No. 20380) and valbenazine (Item No. 26809).1 It is selective for VMAT2 over a panel of 80 receptors at 10 µM.2 NBI 98782 (10 mg/kg) decreases dopamine, serotonin (5-HT), and norepinephrine levels and increases 3,4-dihydroxyphenylacetic acid (DOPAC), homovanillic acid (HVA), and 5-hydroxyindoleacetic acid (5-HIAA) levels in the mouse medial prefrontal cortex.3 It induces ptosis and increases serum prolactin levels in rats when administered at a dose of 10 mg/kg.2 NBI 98782 (10 mg/kg) inhibits PCP- and amphetamine-induced hyperactivity in mice.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yao, Z., Wei, X., Wu, X., et alPreparation and evaluation of tetrabenazine enantiomers and all eight stereoisomers of dihydrotetrabenazine as VMAT2 inhibitors. Eur. J. Med. Chem. 46(5), 1841-1848 (2011).

    2. Grigoriadis, D.E., Smith, E., Hoare, S.R.J., et alPharmacologic characterization of valbenazine (NBI-98854) and its metabolites. J. Pharmacol. Exp. Ther. 361(3), 454-461 (2017).

    3. Huang, M., He, W., Rajagopal, L., et alEffects of NBI-98782, a selective vesicular monoamine transporter 2 (VMAT2) inhibitor, on neurotransmitter efflux and phencyclidine-induced locomotor activity: Relevance to tardive dyskinesia and antipsychotic action. Pharmacol. Biochem. Behav. 190:172872, (2020).