生物活性

• 描述Amisulpride as a specific dopamine receptor antagonist with high and similar affinity for the dopamine D2 and D3 receptor. In vitro, amisulpride has high affinity and selectivity for the human dopamine D2 (Ki = 2.8 nM) and D3 (Ki = 3.2 nM) receptors. Amisulpride has high affinity and selectivity for the human dopamine D2 (Ki = 2.8 nM) and D3 (Ki = 3.2 nM) receptors. At low doses (< or = 10 mg/kg) amisulpride preferentially blocks presynaptic dopamine autoreceptors that control dopamine synthesis and release in the rat, whereas at higher doses (40-80 mg/kg) postsynaptic dopamine D2 receptor occupancy and antagonism is apparent^[3]. Amisulpride has an antidepressant like activity comparable to that of olanzapine though the activity was significantly less than that of fluoxetine^[4]. Amisulpride 400 to 800 mg/day was more effective than haloperidol, risperidone and flupenthixol in controlling affective symptoms in these patients. In randomised, double-blind trials involving patients with predominantly negative symptoms of schizophrenia, amisulpride 50 to 300 mg/day was more effective than placebo. Amisulpride is effective as maintenance therapy in patients with chronic schizophrenia. Long-term treatment with amisulpride was associated with improvements in quality of life and social functioning. Amisulpride is generally well tolerated^[5]. Low-dose amisulpride is effective and well tolerated as a treatment for VLOSLP (Very late-onset (aged ≥ 60 years) schizophrenia-like psychosis), with benefits maintained by prolonging treatment. Potential adverse events include clinically significant extrapyramidal symptoms and falls^[6].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01323205	Schizophrenia	Phase 2	Completed	-	Austria ... more >> Innsbruck, Austria Salzburg, Austria Wien, Austria Belgium Dave, Belgium Duffel, Belgium Kortenberg, Belgium Lede, Belgium Bulgaria Plovdiv, Bulgaria Radnevo N/A, Bulgaria Germany Berlin, Germany Hamburg, Germany Mainz, Germany Mannheim, Germany München, Germany Romania Arad, Romania Brasov, Romania Iasi, Romania Sibiu, Romania Spain Barcelona, Spain Zamora, Spain Collapse <<
  NCT02374567	Dementia Depr... more >>ession Schizophrenia Psychosomatic Disorders Anxiety Disorders Collapse <<	Phase 3	Terminated	-	Germany ... more >> Bezirkskrankenhaus Augsburg Augsburg, Germany Krankenhaus Hedwigshöhe Berlin, Germany Hannover Medical School Hannover, Germany, 30625 Asklepios Fachklinikum Lübben Lübben, Germany Asklepios Fachklinikum Teupitz Teupitz, Germany Collapse <<
  NCT02855229	-	-	Recruiting	March 2020	United States, Massachusetts ... more >> McLean Hospital Recruiting Belmont, Massachusetts, United States, 02478 Contact: David J Crowley, ALM    800-333-0338 ext 4432    neurolab@mclean.harvard.edu    Principal Investigator: Diego A Pizzagalli, PhD Collapse <<

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• 参考文献

• [1] Sarkhel S, Praharaj SK, et al. Amisulpride-induced macrocytic anemia. J Neuropsychiatry Clin Neurosci. 2013 Winter;25(1):E10-1.

  [2] Schoemaker H, Claustre Y, et al. Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity. J Pharmacol Exp Ther. 1997 Jan;280(1):83-97.

  [3] Schoemaker H, Claustre Y, Fage D, et al. Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity. J Pharmacol Exp Ther. 1997;280(1):83‐97

  [4] Pawar GR, Agrawal RP, Phadnis P, Paliwal A, Vyas S, Solanki P. Evaluation of antidepressant like property of amisulpride per se and its comparison with fluoxetine and olanzapine using forced swimming test in albino mice. Acta Pol Pharm. 2009;66(3):327‐331

  [5] Curran MP, Perry CM. Amisulpride: a review of its use in the management of schizophrenia. Drugs. 2001;61(14):2123‐2150

  [6] Reeves S, Eggleston K, Cort E, et al. Therapeutic D2/3 receptor occupancies and response with low amisulpride blood concentrations in very late-onset schizophrenia-like psychosis (VLOSLP). Int J Geriatr Psychiatry. 2018;33(2):396‐404

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