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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Monoamine Transporter-NBI-98782
NBI-98782

Chemical Structure : NBI-98782

CAS No.: 85081-18-1

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

货号: 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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10 mg ¥2980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 551.7
分子式 C29H45NO7S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
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

参考文献

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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