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Levosulpiride

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Chemical Structure| 23672-07-3 同义名 : 左舒必利 ;RV-12309;S-(-)-Sulpiride;Nexipride;(S)-(-)-Sulpiride
CAS号 : 23672-07-3
货号 : A115342
分子式 : C15H23N3O4S
纯度 : 99+%
分子量 : 341.426
MDL号 : MFCD00055220
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
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

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].
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 - -
实验方案
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
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