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左旋舒必利 /Levosulpiride {[allProObj[0].p_purity_real_show]}

货号：A115342 同义名： 左舒必利 / RV-12309;S-(-)-Sulpiride

Levosulpiride, an atypical antipsychotic, can selectively inhibit D2 receptor and it is the (S)-enantiomer of sulpiride.

Levosulpiride 化学结构 CAS号：23672-07-3
Levosulpiride 化学结构
CAS号：23672-07-3
Levosulpiride 3D分子结构
CAS号：23672-07-3
Levosulpiride 化学结构 CAS号：23672-07-3
Levosulpiride 3D分子结构 CAS号：23672-07-3
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Levosulpiride 纯度/质量文件 产品仅供科研

货号：A115342 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 D1 receptor ↓ D2 receptor ↓ D3 receptor ↓ D4 receptor ↓ D5 receptor ↓ DAT ↓ Dopamine receptor ↓ 其他靶点 纯度
Penfluridol +

Dopamine receptor, Ki: 1.6 μM

 		98%
Ansofaxine HCl ++

Dopamine receptor, IC50: 491 nM

 		98%
Tetrahydroberberine,THB +

D2 receptor, pKi: 6.08

 		98+%
Prochlorperazine Maleate ✔ 95%
Olanzapine ✔ 99+%
Trifluoperazine ++++

Dopamine D2 receptor, IC50: 1.1 nM

 		98%
Ropinirole hydrochloride ++

D2 receptor, Ki: 29 nM

 		99%
Lurasidone ++++

D2 receptor, Ki: 1 nM

 		98%
Levosulpiride ✔ 99+%
Pridopidine ✔ 95%
Metoclopramide ✔ ✔ 99+%
Molindone HCl ✔ 98%
Sulpiride ✔ 99+%
Perospirone ++++

D2 receptor, Ki: 1.4 nM

 		99%
Perospirone HCl ++++

D2 receptor, Ki: 1.4 nM

 		98+%
Phenothiazine ✔ 98%
Pimozide +

Dopamine D1 receptor, Ki: 6600 nM

 		+++

Dopamine D2 receptor, Ki: 3.0 nM

 		++++

Dopamine D3 receptor, Ki: 0.83 nM

 		98%
Rotundine ++

D1 receptor, IC50: 166 nM

 		+

D2 receptor, IC50: 1.47 μM

 		+

D3 receptor, IC50: 3.25 μM

 		98%
Domperidone ✔ 99+%
ONC206 ✔ 97%
Pimethixene maleate ++

Dopamine D1 Receptor, pKi: 6.37

 		+++

Dopamine D2 Receptor, pKi: 8.19

 		++

Dopamine D4.4 Receptor, pKi: 7.54

 		97%
Loxapine succinate ++

D1 receptor (human), Ki: 26 nM

D2 receptor (Human), Ki: 62 nM

 		++

D2 receptor (human), Ki: 24 nM

D2 receptor (bovine), Ki: 26 nM

 		+++

D4 receptor (human), Ki: 7.5 nM

 		99%
Chlorprothixene +++

D1 receptor, Ki: 18 nM

 		+++

D2 receptor, Ki: 2.96 nM

 		+++

D3 receptor, Ki: 4.56 nM

 		+++

D5 receptor, Ki: 9 nM

 		98%
SCH-23390 HCl ++++

D1 dopamine receptor, Ki: 0.2 nM

 		++++

D5 dopamine receptor, Ki: 0.3 nM

 		98%
MPP+ iodide ✔ 97%
σ1 Receptor antagonist-1 +

DAT, pKi: 5.8

 		97%
Benztropine mesylate ++

DAT, IC50: 118 nM

 		98%
Azaperone ✔ 98%
Ziprasidone HCl ✔ 98+%
Paliperidone ✔ 98%
Alizapride HCl ✔ 99+%
Amisulpride ✔ 98%
Quetiapine hemifumarate ✔ Adrenergic Receptor 98%
Clozapine N-oxide ✔ 99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Levosulpiride 生物活性

靶点

  • D2 receptor
描述 Levosulpiride, a newer prokinetic agent, selectively inhibits gut and central D2 receptors and is associated with various movement disorders like- tremor, Parkinsonism, dyskinesias and rarely dystonia[3]. Dopamine is the main endogenous inhibitor of prolactin synthesis and secretion in the anterior pituitary. Levosulpiride causes significant elevation of serum prolactin levels in significant number of patients[4]. Levosulpiride appears to be a well-tolerated and effective drug for the treatment for SDs (somatoform disorders). Levosulpiride significantly reduced the number of SD symptoms compared to placebo (P =0.007) after 4 weeks of treatment. Levosulpiride also determined a more evident reduction of the total number of SD symptoms compared to placebo[5]. Levosulpiride frequently causes drug-induced movement disorders, presenting mainly with LIP followed by lower face dyskinesia. The symptoms are often severe, and irreversible even after the withdrawal of levosulpiride[6].

Levosulpiride 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03161652 Diabetic Macular Edema ... 展开 >> Diabetic Retinopathy 收起 << Phase 2 Recruiting December 2020 Mexico ... 展开 >> Instituto Mexicano de Oftalmologia (IMO) Recruiting Queretaro, Mexico, 76090 Contact: Renata Garcia Franco, M.D.    52442 229 0776    renatagarciafranco@gmail.com    Contact: Ellery Lopez Star, M.D.    52442 229 0776    ellerylopezstar@gmail.com    Principal Investigator: Renata Garcia Franco, M.D.          Sub-Investigator: Ximena Mira Lorenzo, M.D.          Sub-Investigator: Paulina Ramirez Neira, M.D.          Sub-Investigator: Carlos D Nuñez Amaro, B.Sc. 收起 <<
NCT00866645 Agitation Phase 2 Phase 3 Completed - China, Hebei ... 展开 >> Hebei Mental Health Center Baoding, Hebei, China, 071000 China, Jiangsu Nanjing Brain Hospital Nanjing, Jiangsu, China, 210029 China, Shaanxi Xi'an Mental Health Center Xi'an, Shaanxi, China, 710061 China, Shanghai Shanghai Mental Health Center Shanghai, Shanghai, China, 200030 China, Yunnan The First Affilliated Hospital Of Kunming Medical College Kunming, Yunnan, China, 650032 收起 <<
NCT02481583 Dyspepsia Phase 1 Completed - -

Levosulpiride 参考文献

[1]Lavania S, Praharaj SK, et al. Efficacy and Safety of Levosulpiride Versus Haloperidol Injection in Patients With Acute Psychosis: A Randomized Double-Blind Study. Clin Neuropharmacol. 2016 Jul-Aug;39(4):197-200.

[2]Garg S, Goyal N, et al. Levosulpiride-induced rabbit syndrome. Aust N Z J Psychiatry. 2013 Mar;47(3):288-9.

[3]Radhakrishnan DM, Goyal V. Levosulpiride-Induced Dystonia: 7 Cases. J Assoc Physicians India. 2018;66(6):95‐96

[4]Kuchay MS, Mithal A. Levosulpiride and Serum Prolactin Levels. Indian J Endocrinol Metab. 2017;21(2):355‐358

[5]Altamura AC, Di Rosa A, Ermentini A, et al. Levosulpiride in somatoform disorders: A double-blind, placebo-controlled cross-over study. Int J Psychiatry Clin Pract. 2003;7(3):155‐159

[6]Shin HW, Kim MJ, Kim JS, Lee MC, Chung SJ. Levosulpiride-induced movement disorders. Mov Disord. 2009;24(15):2249‐2253

Levosulpiride 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.93mL

0.59mL

0.29mL

14.64mL

2.93mL

1.46mL

29.29mL

5.86mL

2.93mL

Levosulpiride 技术信息

CAS号23672-07-3
分子式C15H23N3O4S
分子量 341.426
别名 左舒必利 ;RV-12309;S-(-)-Sulpiride;Nexipride;(S)-(-)-Sulpiride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature
溶解度

DMSO: 50 mg/mL(146.44 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 13 mg/mL clear

PO 0.5% CMC-Na 40 mg/mL suspension

Tags: Levosulpiride | 23672-07-3 | RV-12309 | S-(-)-Sulpiride | RV12309 | RV 12309 | Dopamine Receptor Antagonist | GPCR/G Protein | Neuronal Signaling | Dopamine Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Levosulpiride 纯度/质量文件 | Levosulpiride 亚型比较 | Levosulpiride 生物活性 | Levosulpiride 临床数据 | Levosulpiride 参考文献 | Levosulpiride 实验方案 | Levosulpiride 技术信息

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