产品说明书

Sulpiride

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Chemical Structure| 15676-16-1 同义名 : (±)-舒必利 ;rac-Sulpiride;Dolmatil;Equilid;Enimon;CCRIS-4248;(S)-Sulpiride;(RS)-(±)-Sulpiride;RD 1403;(±)-Sulpiride;Dogmatil;Aiglonyl;Sulpyrid;Dobren
CAS号 : 15676-16-1
货号 : A508747
分子式 : C15H23N3O4S
纯度 : 99+%
分子量 : 341.426
MDL号 : MFCD00055061
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: 105 mg/mL(307.53 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：
生物活性
靶点

  • D2 receptor
描述 Sulpiride is a substituted benzamide with selective dopaminergic blocking activity. Sulpiride was selective for dopamine (D)2 receptors and also blocks D3 and D4 receptors. Sulpiride does not block D1, adrenergic, cholinergic, gamma-aminobutyric acid-ergic, histaminergic, or serotonergic receptors to an appreciable extent. The oral bioavailability of sulpiride is poor, with estimates approximating 35%. Sulpiride may cause extrapyramidal effects, autonomic effects, tardive dyskinesia, and the neuroleptic malignant syndrome[3]. At low dosages (50 to 150 mg/day), sulpiride produces a disinhibiting and antidepressant effect, which is probably related to its action on D2 presynaptic autoreceptors, thus facilitating dopaminergic neurotransmission[4]. Sulpiride and melatonin reduce tinnitus perception, decreasing dopamine activity[5]. Sulpiride attenuated by 36% the anorexia produced by intrahypothalamic injections of amphetamine[6].
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]Lai EC, Hsieh CY, et al. Detecting potential adverse reactions of sulpiride in schizophrenic patients by prescription sequence symmetry analysis. PLoS One. 2014 Feb 27;9(2):e89795.

[2]Nakazato T, Horikawa HP, et al. The dopamine D2 receptor antagonist sulpiride causes long-lasting serotonin release. Eur J Pharmacol. 1998 Dec 11;363(1):29-34.

[3]Caley CF, Weber SS. Sulpiride: an antipsychotic with selective dopaminergic antagonist properties. Ann Pharmacother. 1995 Feb;29(2):152-60

[4]Mauri MC, Bravin S, Bitetto A, Rudelli R, Invernizzi G. A risk-benefit assessment of sulpiride in the treatment of schizophrenia. Drug Saf. 1996 May;14(5):288-98

[5]Lopez-Gonzalez MA, Santiago AM, Esteban-Ortega F. Sulpiride and melatonin decrease tinnitus perception modulating the auditolimbic dopaminergic pathway. J Otolaryngol. 2007 Aug;36(4):213-9

[6]Parada MA, Hernandez L, Hoebel BG. Sulpiride injections in the lateral hypothalamus induce feeding and drinking in rats. Pharmacol Biochem Behav. 1988 Aug;30(4):917-23