NBI-98782
(Synonyms: (+)-α-二氢丁苯那嗪; (+)-DTBZ; (+)-α-Dihydrotetrabenazine; (+)-α-DHTBZ) 目录号 : GC36705
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NBI-98782是一种强效且选择性的vesicular monoamine transporter 2 (VMAT2)抑制剂，Ki值为3nM。
Cas No.:85081-18-1
Sample solution is provided at 25 µL, 10mM.
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NBI-98782 is a potent and selective vesicular monoamine transporter 2 (VMAT2) inhibitor with a Ki value of 3nM [1]. NBI-98782 reduces the packaging of monoamines by targeting VMAT2, thereby leading to a decrease in monoamine release and neural transmission[2]. NBI-98782 has been widely used to promote ptosis in rats, stimulate prolactin secretion, and regulate neural functions[3].
In vivo, NBI-98782 treatment via oral administration at a dose of 10mg/kg/day for 7 days significantly decreased basal levels of dopamine and serotonin, and enhanced the release of acetylcholine and GABA levels in mice [4].
References:
[1] Meyer J M. Valbenazine for tardive dyskinesia[J]. Curr Psychiatr, 2017, 16(5): 40-46.
[2] Terry-Lorenzo R, Albrecht D, Crouch S, et al. Quantifying VMAT2 target occupancy at effective valbenazine doses and comparing to a novel VMAT2 inhibitor: a translational PET study[J]. Neuropsychopharmacology, 2025, 50(7): 1093-1101.
[3] Grigoriadis D E, Smith E, Hoare S R J, et al. Pharmacologic characterization of valbenazine (NBI-98854) and its metabolites[J]. The Journal of Pharmacology and Experimental Therapeutics, 2017, 361(3): 454-461.
[4] Huang M, He W, Rajagopal L, et al. Effects 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[J]. Pharmacology Biochemistry and Behavior, 2020, 190: 172872.
NBI-98782是一种强效且选择性的vesicular monoamine transporter 2 (VMAT2)抑制剂，Ki值为3nM[1]。NBI-98782通过靶向VMAT2减少单胺的包装，从而导致单胺释放和神经传递减少[2]。NBI-98782已被广泛用于诱导大鼠上睑下垂、刺激催乳素分泌和调节神经功能[3]。
在体内，通过口服给予10mg/kg/day剂量的NBI-98782处理7天，显著降低了小鼠的多巴胺和血清素基础水平，并增强了乙酰胆碱的释放和GABA水平[4]。
| Animal experiment [1]: | |
Animal models | Male C57BL/6 J mice |
Preparation Method | Male C57BL/6 J mice, weighing 20-25g, were group housed (four per cage) in a controlled environment held at 21±2°C and 50±15% relative humidity on a 14/10h light-dark cycle. Food and water were available ad libitum. NBI-98782 and tetrabenazine were dissolved in 30% propylene glycol and 20% polyethylene glycol 400 in 0.25% methyl cellulose (400cps) in water. NBI-98782 was orally administered (10mg/kg/day) for 7 days. Microdialysis was performed on the 8th day. |
Dosage form | 10mg/kg/day for 7 days; p.o. |
Applications | NBI-98782 treatment significantly decreased basal levels of dopamine and serotonin, with a trend to decrease norepinephrine levels in mice. |
References: | |
| Cas No. | 85081-18-1 | SDF | |
| 别名 | (+)-α-二氢丁苯那嗪; (+)-DTBZ; (+)-α-Dihydrotetrabenazine; (+)-α-DHTBZ | ||
| Canonical SMILES | COC(C=C1CCN2C[C@@H](CC(C)C)[C@@H]3O)=C(C=C1[C@]2(C3)[H])OC | ||
| 分子式 | C19H29NO3 | 分子量 | 319.44 |
| 溶解度 | DMSO: 33.33 mg/mL (104.34 mM) | 储存条件 | Store at -20°C; protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1305 mL | 15.6524 mL | 31.3048 mL |
| 5 mM | 626.1 μL | 3.1305 mL | 6.261 mL |
| 10 mM | 313 μL | 1.5652 mL | 3.1305 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet