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更新于：2025-07-21
Sulpiride
舒必利
更新于：2025-07-21
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CTR20242937
舒必利片在健康受试者中的随机、开放、单剂量、双周期、自身交叉、空腹及餐
后状态下生物等效性试验
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
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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7,107
项与 舒必利 相关的文献（医药）2025-11-01NEUROPHARMACOLOGY
Transient receptor potential vanilloid 2 (TRPV2) channels modulate the nigrostriatal dopaminergic activity in rats
Article
作者: Mitra, Saptarsi ; Srivastava, Abhinav ; Pradhan, Pritiusha ; Dudhabhate, Biru B ; Basu, Sumela ; Singru, Praful S ; Kokare, Dadasaheb M ; Goswami, Chandan
Thermosensitive TRPV1-4-channels have emerged as novel regulators of neuronal function and behaviour. In midbrain, while TRPV1/TRPV3 regulates ventral tegmental area dopamine (DA) (VTADA) neurons, TRPV1/TRPV3/TRPV4 play a role in the modulation of substantia nigra DA (SNDA) neurons. Although TRPV2 is widely expressed in the brain, its significance in the regulation of VTADA/SNDA neurons is unclear. Herein, we test the occurrence of TRPV2 in midbrain and probe its relevance in the modulation of the nigrostriatal-DAergic pathway in male rats. PCR analysis detected Trpv2 mRNA expression in the midbrain and anti-TRPV2 specific antiserum distinctly labelled neurons in the VTA, SN-pars compacta (SNc), and other midbrain nuclei. Tyrosine hydroxylase (TH) and TRPV2 were co-expressed in the VTA and SNc neurons with the latter displaying especially high TRPV2-enrichment. The SNc TH neurons projecting to the dorsal striatum co-expressed TRPV2. While intra-SNc administration of TRPV2-agonist probenecid increased the locomotor activity, pre-treatment with intra-SNc TRPV2-antagonist SET2 or intra-dorsal striatum DA-D2-receptor antagonist, sulpiride blocked the probenecid-induced response. In ex-vivo midbrain slices, probenecid treatment enhanced TH-ir and [Ca2+]i levels in SNc. Pre-treatment with SET2 blocked probenecid-induced changes in TH-ir. We next examined whether probenecid alters the striatal DA-levels during progressive degeneration of the nigrostriatal-DAergic pathway. In 6-hydoxydopamine (6-OHDA)-treated rats, probenecid/SET2 were injected intra-SNc and the changes in striatal-DA levels were analyzed. While intra-SNc probenecid enhanced striatal-DA levels, pre-treatment with SET2 reduced PB-induced response. We suggest TRPV2 as a novel regulator of the nigrostriatal-DAergic pathway and a potential target for the treatment of Parkinson's disease.
2025-08-01NEUROPHARMACOLOGY
Aripiprazole: The antiallodynic and antihyperalgesic effects in chronic constriction injury-induced neuropathic pain and reserpine-induced fibromyalgia with possible mechanisms
Article
作者: Arslan, Rana ; Aykaç, Özlem ; Bektas, Nurcan ; Okcay, Yagmur
Neuropathic pain, caused by peripheral or central nerve damage, and fibromyalgia, a chronic musculoskeletal disorder, require complex treatment approaches. This study evaluated the antiallodynic and antihyperalgesic effects of aripiprazole (1, 5, and 10 mg/kg, i. p.) in rats with chronic constriction injury-induced neuropathic pain and reserpine-induced fibromyalgia in female Sprague-Dawley rats, using electronic von Frey and Hargreaves tests. Dopaminergic, serotonergic, and opioidergic systems' roles were assessed through pre-treatment with sulpiride (50 mg/kg), WAY 100635 (1 mg/kg), and naloxone (1 mg/kg), respectively. The effect of aripiprazole was compared with 30 mg/kg pregabalin in the neuropathic pain model and 30 mg/kg duloxetine in the fibromyalgia model. Aripiprazole demonstrated significant antiallodynic and antihyperalgesic activity in both models. It did not change locomotor activity at a dose of 1 mg/kg but caused a decrease at a dose of 5 mg/kg. Dopamine D2, serotonin 5-HT1A, and opioidergic receptors contributed to aripiprazole's effects at varying levels. This study highlights the potential use of aripiprazole for managing neuropathic pain and fibromyalgia by targeting multiple receptor systems. The findings demonstrate the potential use of aripiprazole alone or as an adjuvant in the treatments of neuropathic pain and fibromyalgia.
2025-07-11JOURNAL OF ORGANIC CHEMISTRY
Photoredox-Catalyzed Three-Component Assembly of Primary Aryl Sulfonamides Using (NH4)2CO3: Late-Stage Drug Sulfonamidation
Article
作者: Sui, Xianwei ; Song, Man ; Liu, Feiyang ; Ma, Xiaoxu ; Liu, Binjie ; Liu, Xinyue ; Ma, Mengxue ; Bi, Yue ; Yan, Fengying ; Liu, Lingling
Primary aryl sulfonamides feature prominently in medicinal chemistry and organic synthesis. Herein, a metal-free photoredox-catalyzed three-component assembly of primary aryl sulfonamides via an aryl sulfonyl ammonium trifluoromethanesulfonate intermediate has been described. A variety of structurally diverse primary aryl sulfonamides were synthesized rapidly from dibenzothiophenium (DBT) salts under simple and mild conditions using (NH4)2CO3 as the nucleophile. Notably, this methodology can be employed as an efficient and sustainable approach for late-stage drug sulfonamidation. Broad functional group tolerance is a feature of this methodology. Moreover, the method was applied to the total synthesis of sulpiride to showcase its synthetic utility.
100 项与 舒必利 相关的药物交易
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研发状态
批准上市
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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 |
未上市
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 糖尿病性视网膜病变 | 临床前 | 墨西哥 | 2020-06-01 |
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临床结果
临床结果
适应症
分期
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N/A | - | Sulpiride-treated group | 廠蓋壓鹽鑰積鏇糧餘廠(夢壓鑰鹽憲觸糧衊膚艱) = 衊鹽餘蓋餘鑰膚醖構夢 獵範鬱膚廠積範築膚選 (齋鑰鑰鹹醖廠繭選廠醖 ) | - | 2020-09-12 | ||
廠蓋壓鹽鑰積鏇糧餘廠(夢壓鑰鹽憲觸糧衊膚艱) = 壓鹽顧鹽餘選齋製鏇糧 獵範鬱膚廠積範築膚選 (齋鑰鑰鹹醖廠繭選廠醖 ) | |||||||
N/A | 糖尿病性视网膜病变 prolactin | - | 遞齋襯夢膚觸鹽鹽範壓(製獵鹹壓鏇衊構積膚獵) = reduced diabetes-induced retinal vasopermeability 獵艱鏇艱選顧鹽憲鬱齋 (壓窪餘鹽願繭淵獵觸網 ) | - | 2020-06-01 | ||
(Control (non-diabetic)) | |||||||
N/A | - | 醖願願夢廠願簾淵鏇網(夢夢遞積艱膚廠鑰繭蓋) = 齋鏇選醖鏇鹹夢膚鹽餘 廠艱糧淵糧壓繭壓觸簾 (築鑰積糧選壓夢膚鹽糧 ) | - | 2018-10-01 | |||
Flupenthixol melitracen | 醖願願夢廠願簾淵鏇網(夢夢遞積艱膚廠鑰繭蓋) = 膚壓獵鹽艱淵鬱餘簾顧 廠艱糧淵糧壓繭壓觸簾 (築鑰積糧選壓夢膚鹽糧 ) |
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