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Sulpiride/舒必利 {[allProObj[0].p_purity_real_show]}

货号:A508747 同义名: (±)-舒必利 / rac-Sulpiride; Dolmatil

Sulpiride是一种典型的抗精神病药,通过结合多巴胺D2受体发挥作用,常用于研究精神分裂症和抑郁症。

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Sulpiride/舒必利 化学结构 CAS号:15676-16-1
Sulpiride/舒必利 化学结构
CAS号:15676-16-1
Sulpiride/舒必利 3D分子结构
CAS号:15676-16-1
Sulpiride/舒必利 化学结构 CAS号:15676-16-1
Sulpiride/舒必利 3D分子结构 CAS号:15676-16-1
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Sulpiride/舒必利 纯度/质量文件 产品仅供科研

货号:A508747 标准纯度: {[allProObj[0].p_purity_real_show]}
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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

99%
Tetrahydroberberine +

D2 receptor, pKi: 6.08

98+%
Prochlorperazine Maleate 98% (HPLC)
Olanzapine 99+%
Trifluoperazine ++++

Dopamine D2 receptor, IC50: 1.1 nM

98%
Ropinirole HCl ++

D2 receptor, Ki: 29 nM

99%
Lurasidone ++++

D2 receptor, Ki: 1 nM

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

D2 receptor, Ki: 1.4 nM

99%
Perospirone HCl ++++

D2 receptor, Ki: 1.4 nM

99%
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 99%
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

98%
Chlorprothixene +++

D1 receptor, Ki: 18 nM

+++

D2 receptor, Ki: 2.96 nM

+++

D3 receptor, Ki: 4.56 nM

+++

D5 receptor, Ki: 9 nM

99%
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。

Sulpiride/舒必利 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].

Sulpiride/舒必利 细胞实验

Cell Line
Concentration Treated Time Description References
HCMEC/D3 cells 1, 5, 25 µM 2 minutes To study the transport of Sulpiride in brain microvascular endothelial cells, results showed a carrier-mediated uptake mechanism AAPS J. 2014 Nov;16(6):1247-58.
MDA-MB-231 cells 50 µM 48 hours To evaluate the effect of sulpiride and dexamethasone combination on colony formation, results showed the combination significantly inhibited colony formation Acta Pharmacol Sin. 2017 Sep;38(9):1282-1296.
4T1 cells 50 µM 48 hours To evaluate the effect of sulpiride and dexamethasone combination on colony formation, results showed the combination significantly inhibited colony formation Acta Pharmacol Sin. 2017 Sep;38(9):1282-1296.

Sulpiride/舒必利 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Rats MAM-E17 schizophrenia model rats Bilateral microinjection into the ventral pallidum 0.1 μg, 1.0 μg, 4.0 μg Single administration To investigate the effects of sulpiride on locomotor activity and conditioned place preference in MAM-E17 rats. The results showed that larger doses of sulpiride reduced locomotor activity and restored habituation disturbance in MAM-E17 animals. Additionally, the largest dose of sulpiride induced CPP in SAL-E17 animals but not in MAM-E17 animals. Sci Rep. 2024 May 29;14(1):12305
Wistar rats Ventral pallidum microinjection model Bilateral ventral pallidum microinjection 0.1 μg, 1.0 μg, and 4.0 μg per side Single injection followed by behavioral observation To investigate the effects of sulpiride on spatial learning and conditioned place preference. Results showed that intra-VP sulpiride dose-dependently impairs learning processes, but the largest dose induces place preference. Sci Rep. 2022 Nov 10;12(1):19247
Zebrafish Cocaine-induced conditioned place preference model Water exposure 10 μM 45 minutes exposure followed by behavioral testing To investigate the effect of sulpiride on cocaine-induced conditioned place preference. Results showed that sulpiride completely blocked cocaine-induced CPP. Pharmacol Biochem Behav. 2012 Dec;103(2):157-67
Sprague-Dawley rats Healthy rats Oral 15 mg/kg Single dose To evaluate the pharmacokinetic parameters of sulpiride lipospheres, showing a 3.4-fold improvement in oral bioavailability Int J Nanomedicine. 2021 Mar 9;16:2013-2044
Zebrafish (AB strain) Zebrafish Water exposure 20 ng/L, 50 ng/L, 100 ng/L Half of the water replaced daily for 14 days To investigate the effects of sulpiride and clozapine on dopaminergic (DAergic) and serotonergic (5-HTergic) neurotransmitter systems in the brain of zebrafish. Results showed that sulpiride and clozapine interfered with DAergic and 5-HTergic neurotransmitter systems in the telencephalon and diencephalon of zebrafish, leading to abnormal mRNA and protein levels of key functional molecules in DA and 5-HT signaling pathways. Sci Rep. 2022 Oct 26;12(1):17973
Nude mice Human breast cancer MCF-7/Adr xenograft model Oral 25 or 50 mg/kg Daily administration SUL significantly enhanced the inhibitory effect of DEX on the growth of drug-resistant breast cancer by antagonizing D2DR, indicating the involvement of a CSC-related mechanism Acta Pharmacol Sin. 2019 Dec;40(12):1596-1602
C57BL/6J mice Brain slice model Recirculating perfusion 5 μM Single 50 ms flash Block D2 receptors and measure dopamine dissociation rates ACS Chem Neurosci. 2020 Mar 18;11(6):939-951

Sulpiride/舒必利 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

Sulpiride/舒必利 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

Sulpiride/舒必利 技术信息

CAS号15676-16-1
分子式C15H23N3O4S
分子量 341.43
SMILES Code O=C(NCC1N(CC)CCC1)C2=CC(S(=O)(N)=O)=CC=C2OC
MDL No. MFCD00055061
别名 (±)-舒必利 ;rac-Sulpiride; Dolmatil; Equilid; Enimon; CCRIS-4248; (S)-Sulpiride; (RS)-(±)-Sulpiride; RD 1403; (±)-Sulpiride; Dogmatil; Aiglonyl; Sulpyrid; Dobren
运输蓝冰
InChI Key BGRJTUBHPOOWDU-UHFFFAOYSA-N
Pubchem ID 5355
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, room temperature

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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