预约演示
更新于：2025-04-05
Sulpiride
舒必利
更新于：2025-04-05
概要
基本信息
非在研机构- |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C15H23N3O4S |
InChIKeyBGRJTUBHPOOWDU-UHFFFAOYSA-N |
CAS号15676-16-1 |
关联
18
项与 舒必利 相关的临床试验NCT05208294
The Role of Dopamine, Reward Learning and Prefrontal Activity in Expectation-induced Mood Enhancement
NCT05884671
Dopaminergic Mechanisms of Gating Working Memory, Learning and Motivation: a Pharmaco-fMRI Study
ACTRN12620000075987
The role of dopamine: Investigating the impact of Sulpiride exposure on exercise-related enhancement of motor skill learning in healthy volunteers.
100 项与 舒必利 相关的临床结果
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100 项与 舒必利 相关的转化医学
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100 项与 舒必利 相关的专利（医药）
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6,643
项与 舒必利 相关的文献（医药）2025-05-24Journal of biomolecular structure & dynamics
Monophasic coamorphous sulpiride: a leap in physicochemical attributes and dual inhibition of GlyT1 and P-glycoprotein, supported by experimental and computational insights
Article
作者: Singh, Shashi Bala ; Khemchandani, Rahul ; Tomar, Devendra Singh ; Bazaz, Mohd Rabi ; Dandekar, Manoj P. ; Samanthula, Gananadhamu ; Pardhi, Ekta ; Mehra, Neelesh Kumar
Study aimed to design and development of a supramolecular formulation of sulpiride (SUL) to enhance its solubility, dissolution and permeability by targeting a novel GlyT1 inhibition mechanism. SUL is commonly used to treat gastric and duodenal ulcers, migraine, anti-emetic, anti-depressive and anti-dyspeptic conditions. Additionally, Naringin (NARI) was incorporated as a co-former to enhance the drug's intestinal permeability by targeting P-glycoprotein (P-gp) efflux inhibition. NARI, a flavonoid has diverse biological activities, including anti-apoptotic, anti-oxidant, and anti-inflammatory properties. This study aims to design and develop a supramolecular formulation of SUL with NARI to enhance its solubility, dissolution, and permeability by targeting a novel GlyT1 inhibition mechanism, extensive experimental characterization was performed using solid-state experimental techniques in conjunction with a computational approach. This approach included quantum mechanics-based molecular dynamics (MD) simulation and density functional theory (DFT) studies to investigate intermolecular interactions, phase transformation and various electronic structure-based properties. The findings of the miscibility study, radial distribution function (RDF) analysis, quantitative simulations of hydrogen/π-π bond interactions and geometry optimization aided in comprehending the coamorphization aspects of SUL-NARI Supramolecular systems. Molecular docking and MD simulation were performed for detailed binding affinity assessment and target validation. The solubility, dissolution and ex-vivo permeability studies demonstrated significant improvements with 31.88-fold, 9.13-fold and 1.83-fold increments, respectively. Furthermore, biological assessments revealed superior neuroprotective effects in the SUL-NARI coamorphous system compared to pure SUL. In conclusion, this study highlights the advantages of a drug-nutraceutical supramolecular formulation for improving the solubility and permeability of SUL, targeting novel schizophrenia treatment approaches through combined computational and experimental analyses.
2025-05-01NEUROBIOLOGY OF LEARNING AND MEMORY
The impact of systemic blockade of dopamine receptors on the acquisition of two-way active avoidance in male rats
Article
作者: Vervliet, B ; Lopez-Moraga, A ; Beckers, T ; Vercammen, L ; Luyten, L
Active threat avoidance is a core aspect of adaptive and maladaptive behavior, yet its underlying mechanisms are not fully understood. Prior studies concluded that pharmacologically blocking dopaminergic receptors (DRs) disrupted avoidance acquisition, but it remains unclear whether such effects on learning persist during a drug-free follow-up test. To assess the involvement of D1R and D2R in avoidance acquisition, we conducted two experiments. In Experiment 1, thirty-six male Wistar rats underwent a single avoidance training session involving 30 tone-shock pairings. Rats could avoid the shock by moving to the opposite compartment of the shuttle box. Twenty minutes before training, rats received either D1R antagonist SCH23390 (0.05 mg/kg), D2R antagonist sulpiride (20 mg/kg), or vehicle. While sulpiride did not affect avoidance, 0.05 mg/kg SCH23390 significantly reduced the number of avoidance responses. In a separate test, 0.05 mg/kg SCH23390 also reduced locomotor activity. In Experiment 2 (N = 24), a lower dose of SCH23390 (0.025 mg/kg) was administered, and a drug-free avoidance test under continued reinforcement was added 24 h later to test for sustained effects of D1R blockade on avoidance in the absence of acute drug effects. Although animals avoided less with SCH23390 in the system, this effect did not persist 24 h later, suggesting that effects of D1R blockade during avoidance training might reflect an acute disruption of secondary processes involved in the performance of avoidance behavior rather than an actual impairment of avoidance learning.
2025-05-01PHYSIOLOGY & BEHAVIOR
Involvement of D2-like dopamine receptors within the ventral tegmental area in the cannabidiol's inhibitory effects on the methamphetamine-seeking behavior
Article
作者: Haghparast, Abbas ; Azizbeigi, Ronak ; Fattahi, Mojdeh ; Ezzati, Mohammad Javad ; Ezzati, Mohammad Reza
Cannabidiol (CBD) is a non-psychoactive substance derived from marijuana. Although a comprehensive understanding of CBD's mechanism of action is still lacking, it is well-established that CBD can effectively mitigate the addictive properties associated with drugs. This study examined how CBD inhibits the acquisition and expression of methamphetamine-induced conditioned place preference (CPP) through D2-like dopamine receptors (D2R) in the ventral tegmental area (VTA). After recovery from surgery, animals were subjected to bilateral intra-VTA administration of different dosages (0.25, 1, and 4 μg/0.3 μl DMSO per side) of a selective D2R antagonist, sulpiride before intracerebroventricular (ICV) injection of CBD, during the conditioning phase (10 μg/5 μl DMSO) or once in the post-conditioning phase (50 μg/5 μl DMSO) of methamphetamine-induced CPP (daily subcutaneous injections of methamphetamine at 1 mg/kg over 5-day conditioning period). Findings revealed that CBD inhibits the acquisition and expression of methamphetamine reward memory. At the same time, microinjection of D2R antagonists into the VTA significantly reduced CBD's suppressive effect on the acquisition (0.25 μg; P<0.05, 1 and 4 μg; P<0.001) and expression (1 and 4 μg; P<0.01) of methamphetamine place preference. Moreover, D2R blockage alone in the VTA did not affect the formation and expression of methamphetamine-induced CPP. In addition, the present study showed that administration of intra-VTA sulpiride and ICV injection of CBD together does not cause place preference in the CPP paradigm. In conclusion, pharmacological manipulation of D2Rs in the VTA may alter CBD's suppressive effects on the methamphetamine-context associations.
100 项与 舒必利 相关的药物交易
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研发状态
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 抑郁症 | 日本 | 1979-08-03 | |
| 精神分裂症 | 日本 | 1979-08-03 | |
| 十二指肠溃疡 | 日本 | 1973-01-13 | |
| 胃溃疡 | 日本 | 1973-01-13 |
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临床结果
临床结果
适应症
分期
评价
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N/A | - | Sulpiride-treated group | 鏇顧構廠構製選艱築醖(艱鹹鹽範鏇構廠範夢夢) = 蓋廠顧衊遞選選齋餘繭 窪網願鬱範積範夢築範 (壓簾鑰壓製廠齋獵壓齋 ) | - | 2020-09-12 | ||
鏇顧構廠構製選艱築醖(艱鹹鹽範鏇構廠範夢夢) = 構網繭範艱淵蓋艱選選 窪網願鬱範積範夢築範 (壓簾鑰壓製廠齋獵壓齋 ) | |||||||
N/A | 糖尿病性视网膜病变 prolactin | - | 顧鏇簾鹽遞構廠淵艱願(襯選齋蓋簾憲鬱艱鹹齋) = reduced diabetes-induced retinal vasopermeability 積選窪遞遞願選願淵衊 (鹽獵廠鑰築醖願範鏇蓋 ) | - | 2020-06-01 | ||
(Control (non-diabetic)) | |||||||
N/A | - | 16 | 糧憲願憲蓋願艱蓋鬱願(醖齋衊襯網鏇壓鬱壓壓) = 餘膚築築襯廠糧鑰膚觸 積蓋鏇艱製選願鬱壓膚 (繭觸鬱艱網製製餘廠鬱 ) 更多 | - | 2013-07-01 |
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