Sultopride (LIN-1418)
(Synonyms: 舒托必利; LIN-1418) 目录号 : GC31188Sultopride (LIN-1418) (LIN-1418) 是多巴胺 D2 受体的选择性拮抗剂。
Cas No.:53583-79-2
Sample solution is provided at 25 µL, 10mM.
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Animal experiment: | Thirty-six male Sprague-Dawley rats weighing 180 to 220 g are used in this study. The rats are divided into three groups of 6 each. One group is intraperitoneally injected with Sultopride (100 mg/kg body weight), the second group with sulphide (100 mg/kg body weight), and the third group with normal saline. One hundred minutes after the initial treatments, apomorphine (0.1 mg/kg body weight, dissolved in saline ad libitum) is administered subcutaneously to the three groups, and 20 minutes later the rats are sacrificed. The third group serves as controls[1]. |
References: [1]. Moriuchi K, et al. Differences in effects of sultopride and sulpiride on dopamine turnover in rat brain. Neurochem Res. 1995 Jan;20(1):95-9. |
Sultopride is a selective antagonist of dopamine D2 receptor.
Sultopride is a selective antagonist of dopamine D2 receptor. DOPAC and HVA levels in the striatum, the nucleus accumbens and the medial prefrontal cortex are higher in the rats treated with Sultopride and sulpiride than those of the controls. In the striatum, DOPAC and HVA levels are higher in the Sultopride-treated rats than the sulpiride-treated rats (p<0.05). In the nucleus accumbens, DOPAC levels are higher in the Sultopride-treated rats than sulpiride treated rats (p<0.05). In the Sultopride-treated rats, DOPAC and HVA levels are higher in the striatum or in the nucleus accumbens than in the medial prefrontal cortex (p<0.05)[1].
[1]. Moriuchi K, et al. Differences in effects of sultopride and sulpiride on dopamine turnover in rat brain. Neurochem Res. 1995 Jan;20(1):95-9.
Cas No. | 53583-79-2 | SDF | |
别名 | 舒托必利; LIN-1418 | ||
Canonical SMILES | O=C(NCC1N(CC)CCC1)C2=CC(S(=O)(CC)=O)=CC=C2OC | ||
分子式 | C17H26N2O4S | 分子量 | 354.46 |
溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.8212 mL | 14.106 mL | 28.2119 mL |
5 mM | 0.5642 mL | 2.8212 mL | 5.6424 mL |
10 mM | 0.2821 mL | 1.4106 mL | 2.8212 mL |
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Burning mouth syndrome: a review and update
Burning mouth syndrome (BMS) is mainly found in middle aged or elderly women and is characterized by intense burning or itching sensation of the tongue or other regions of the oral mucosa. It can be accompanied by xerostomia and dysgeusia. The syndrome generally manifests spontaneously, and the discomfort is typically of a continuous nature but increases in intensity during the evening and at night. Although BMS classically has been attributed to a range of factors, in recent years evidence has been obtained relating it peripheral (sensory C and/or trigeminal nerve fibers) or central neuropathic disturbances (involving the nigrostriatal dopaminergic system). The differential diagnosis requires the exclusion of oral mucosal lesions or blood test alterations that can produce burning mouth sensation. Patient management is based on the avoidance of causes of oral irritation and the provision of psychological support. Drug treatment for burning sensation in primary BMS of peripheral origin can consist of topical clonazepam, while central type BMS appears to improve with the use of antidepressants such as duloxetine, antiseizure drugs such as gabapentin, or amisulpride.
Amisulpride
Current pharmacotherapeutic approaches for dysthymic disorder and persistent depressive disorder
Introduction: Persistent Depressive Disorder (PDD) is a nosological entity introduced with DSM-5, encompassing numerous different conditions including Dysthymia, recurrent Major Depressive Disorder, Double Depression and Chronic Major Depression. PDD is a particularly significant cause of disease burden in the general population. Areas covered: In the present paper, the authors explore the controversies surrounding the definition of PDD, the current approach to its treatment endorsed by the major scientific bodies, along with the available evidence on the efficacy of said treatments. Expert opinion: Clinicians need to be particularly vigilant and always gather a thorough history. In this diagnostic group, there is a relevant risk of having an undiagnosed Bipolar Disorder as affected individuals typically fail to recognize the pathological components of hypomanic episodes. In this setting, it is crucial to reconsider the diagnosis and to frequently verify compliance with the treatment plan. Numerous technological advances, particularly in the neuroimaging field, offer new insight and new challenges in defining the pathophysiological mechanisms of depressive syndromes. In the future, these advances may offer guidance towards an improved treatment approach and diagnostic process.
Amisulpride - is it as all other medicines or is it different? An update
Amisulpride is an antipsychotic available in Europe since 1990s, in Poland since 2000. Subsequent years brought to Polish market more second-generation compounds such as ziprasidone and aripiprazole. In 2018, the Agency for Health Technology Assessment and Tariff System issued positive recommendation for lurasidone in schizophrenia (Recommendation 30/2018) facilitating its entry to the market. Thanks to new molecules, therapeutic possibilities of medicines consequently rise, however, higher number of available substances of different properties brings also more dilemmas which one to pick. Since new publications of comparative drug trials, meta-analyses and systematic reviews are issued regularly, the authors present herein publications issued within last ten years focusing on amisulpride as opposed to other neuroleptics used in Poland. Although in many aspects it is equivalent to other atypical antipsychotics, it still has some advantages. Amisulpride seems to have better outcome than classic and atypical neuroleptics when it comes to depressive symptoms and predominant negative symptoms. It might also be superior to haloperidol in inducing symptomatic remission in first episode schizophrenia. Except for prolactin increase its side effects profile is favorable - it rarely leads to extrapyramidal symptoms (which are dose-dependent) and sedation. Therefore many patients accept treatment with amisulpride for its measurable clinical gains, such as improvement of positive symptoms and higher quality of life, compared to typical neuroleptics. Pharmacokinetics of amisulpride also encourage its wider use, especially when there is either a need for combined psychopharmacotherapy or comorbidity with general medical condition rises a need for somatic parallel treatment.
Amisulpride, aripiprazole, and olanzapine in patients with schizophrenia-spectrum disorders (BeSt InTro): a pragmatic, rater-blind, semi-randomised trial
Background: Amisulpride, aripiprazole, and olanzapine are first-line atypical antipsychotics that have not previously been compared head-to-head in a pragmatic trial. We aimed to compare the efficacy and safety of these agents in a controlled trial.
Methods: This pragmatic, rater-blind, randomised controlled trial was done in three academic centres of psychiatry in Norway, and one in Austria. Eligible patients were aged 18 years or older, met ICD-10 criteria for schizophrenia-spectrum disorders (F20-29), and had symptoms of active psychosis. Eligible patients were randomly assigned to receive oral amisulpride, aripiprazole, or olanzapine. Treatment allocation was open to patients and staff, and starting dose, treatment changes, and adjustments were left to the discretion of the treating physician. Computer-generated randomisation lists for each study centre were prepared by independent statisticians. Patients were followed up for 52 weeks after random assignment, during which assessments were done 8 times by researchers masked to treatment. The primary outcome was reduction of the Positive And Negative Syndrome Scale (PANSS) total score at 52 weeks, and primary analyses were done in the intention-to-treat population. This trial is registered with ClinicalTrials.gov, number NCT01446328.
Findings: Between Oct 20, 2011, and Dec 30, 2016, we assessed 359 patients for eligibility. 215 patients were excluded (107 did not meet inclusion criteria, 82 declined to participate, 26 other reasons). 144 patients (mean baseline PANSS total estimated score 78·4 [SD 1·4]) were randomly assigned 1:1:1 to receive amisulpride (44 patients), aripiprazole (48 patients) or olanzapine (52 patients). After 52 weeks, the patients allocated to amisulpride had a PANSS total score reduction of 32·7 points (SD 3·1) compared with 21·9 points reduction with aripiprazole (SD 3·9, p=0·027) and 23·3 points with olanzapine (2·9, p=0·025). We observed weight gain and increases of serum lipids and prolactin in all groups. 26 serious adverse events (SAEs) among 20 patients were registered (four [9%] of 44 patients allocated to amisulpride, ten [21%] of 48 patients allocated to aripiprazole, and six [12%] of 52 patients allocated to olanzapine), with no statistically significant differences between the study drugs. 17 (65%) of the 26 SAEs occurred during the use of the study drug, with readmission or protracted hospital admission accounting for 13 SAEs. One death by suicide, one unspecified death, and one life-threatening accident occurred during follow-up, after cessation of treatment.
Interpretation: Amisulpride was more efficacious than aripiprazole or olanzapine for reducing the PANSS total scores in adults with schizophrenia-spectrum disorders. Side-effect differences among the groups were generally small. This study supports the notion that clinically relevant efficacy differences exist between antipsychotic drugs. Future research should aim to compare first-line antipsychotics directly in pragmatic clinical trials that reflect everyday clinical practice.
Funding: The Research Council of Norway, the Western Norway Regional Health Trust, and participating hospitals and universities.