Sulpiride | 舒必利

MCE 国际站：Sulpiride

中文名：舒必利

CAS：15676-16-1

品牌：MedChemExpress (MCE)

存储条件：Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.

生物活性：舒必利是一种D2受体α拮抗剂，是苯甲酰胺类的非典型抗精神病药，主要用于治疗与精神分裂症和重度抑郁症相关的精神病，有时小剂量用于治疗焦虑症和轻度抑郁症。

体外：Sulpiride (20-50 μmol/L; 48 h) 在人乳腺癌 MCF-7/Adr 细胞中没有抗肿瘤活性，但可以以剂量依赖的方式降低体外和体内降低了癌症干细胞样细胞 (CSCs) 的比例
[4]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内：Sulpiride ( 50 mg/kg; 皮下注射; 单剂量) 在 Sprague-Dawley 大鼠中能增加大鼠的多巴胺水平
[2]。 Sulpiride (5-20 mg/kg; 腹腔注射; 单剂量) 在帕金森病 (PD) 小鼠中剂量为 20 mg/kg 时会改善小鼠的记忆力但是会诱导焦虑
[3]。 Sulpiride (25-100 mg/kg; 口服; 一天一次连续 18 天) 在携带 MCF-7/Adr 异种移植的 nu/nu 裸鼠中与地塞米松 (DEX) (HY-14648) (1 和 8 mg/kg) 联合使用时可以增强 DEX 的抗肿瘤活性，且对器官没有明显毒性
[4]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Sprague-Dawley rats model
[2] Dosage: 50 mg/kg Administration: Subcutaneous injection (s.c.); Single dose. Result: Caused dopamine concentrations in the dialysates to roughly double. Animal Model: 6-hydroxydopamine (6-OHDA) male NMRI mouse model of Parkinson’s disease (PD)
[3] Dosage: 5 mg/kg, 10 mg/kg, 20 mg/kg Administration: Intraperitoneal injection (i.p.); Single dose Result: Decreased %OAT (open-arm time) but had no significant effect on %OAE (open-arm entries) ａnd locomotor activity. Animal Model: Female nu/nu nude mouse models of breast cancer bearing MCF-7/Adr xenografts
[4] Dosage: 25 mg/kg, 50 mg/kg, 100 mg/kg Administration: Oral gavage (p.o.); Once daily for 18 days. In combination with DEX (1 ａnd 10 mg/kg; p.o.; Once daily for 18 days) Result: When used in combination with DEX (1 mg/kg) at 50 m/kg, enhanced the tumor suppression rate (14.4%). When combined with DEX (8 mg/kg) at 25, 50, ａnd 100 mg/kg, enhanced the tumor suppression rate by 30.2%, 27.55%, ａnd 14.97%, respectively. Clinical Trial

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研究领域：GPCR/G Protein | Neuronal Signaling

作用靶点：Dopamine Receptor

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参考文献：
[1]. Rüther, E et al. Antidepressant action of sulpiride. Results of a placebo-controlled double-blind trial. Pharmacopsychiatry vol. 32,4 (1999): 127-35.
[2]. Jaworski, J N et al. Effect of dopamine D2/D3 receptor antagonist sulpiride on amphetamine-induced changes in striatal extracellular dopamine. European journal of pharmacology vol. 418,3 (2001): 201-6.
[3]. Zarrindast, Mohammad-Reza et al. Synergistic effect between quinpirole ａnd L-NAME as well as sulpiride ａnd L-arginine on the modulation of anxiety ａnd memory processes in the 6-OHDA mouse model of Parkinson＇s disease: An isobologram analysis. Neurobiology of learning ａnd memory vol. 186 (2021): 107538.
[4]. Li, Jian et al. Dopamine D2 receptor antagonist sulpiride enhances dexamethasone responses in the treatment of drug-resistant ａnd metastatic breast cancer. Acta pharmacologica Sinica vol. 38,9 (2017): 1282-1296.