生物活性

• 描述Trimipramine maleate is a 5-HT receptor antagonist, with pKis of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively^[3]. Two week chronic administration of trimipramine increased the brain concentration and metabolism of dopamine and 5-hydroxytryptamine. Trimipramine induces adaptive changes in dopamine and 5-hydroxytryptamine neurotransmission^[4]. With IC50 values between 2 and 10 μM, trimipramine inhibited hSERT(serotonin), hNAT(noradrenaline), hOCT1, and hOCT2 (human organic cation transporters), whereas clearly higher concentrations were needed for half-maximal inhibition of hDAT. Desmethyl-trimipramine showed about the same potencies as trimipramine, whereas 2-hydroxy-trimipramine was less potent at hNAT, hSERT, and hOCT1. Trimipramine-N-oxide preferentially inhibited hSERT^[5]. Trimipramine maleate as a highly effective antidepressant with an efficacy profile similar to the other TCAs (tricyclic antidepressants). Clinically, its anxiolytic and sedative properties distinguish it from most other TCAs. The side effect profile of trimipramine is in some ways similar to those of the tertiary amine TCAs with a preponderance of anticholinergic and sedative effects^[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
  NCT02191358	-	-	Completed	-	United States, California ... more >> Dr. Michael Dao Garden Grove, California, United States, 92844 United States, Colorado Kaiser Permanente Colorado Denver, Colorado, United States, 80011 United States, Kentucky Gill Heart Institute Lexington, Kentucky, United States, 40508 United States, Maryland IRC Clinics Towson, Maryland, United States, 21204 United States, Massachusetts Internal Medicine & Cardiology Associates Fall River, Massachusetts, United States, 02720 Prima CARE Fall River, Massachusetts, United States, 02720 United States, Virginia Carilion Clinic Christiansburg, Virginia, United States, 24073 Collapse <<
  NCT02237937	Major Depression	Phase 4	Unknown	December 2014	Germany ... more >> Max Planck Institute of Psychiatry Recruiting Munich, Bavaria, Germany, 80804 Principal Investigator: Barbara Breitenstein, MSc 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 <<

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• 参考文献

• [1] Trimipramine maleate (Surmontil)--another tricyclic antidepressant. Med Lett Drugs Ther. 1980 Feb 8;22(3):16.

  [2] Goulton J, Baker PG, et al. A multicentre general practice study of 'Surmontil' (trimipramine maleate) in the treatment of endogenous depression with associated sleep disturbances. Br J Clin Pract. 1978 Nov;32(11):323-5.

  [3] Jenck F, Moreau JL, Mutel V, Martin JR, Haefely WE. Evidence for a role of 5-HT1C receptors in the antiserotonergic properties of some antidepressant drugs. Eur J Pharmacol. 1993;231(2):223-229

  [4] Juorio AV, Li XM, Boulton AA. The effects of chronic trimipramine treatment on biogenic amine metabolism and on dopamine D2, 5-HT2 and tryptamine binding sites in rat brain. Gen Pharmacol. 1990;21(5):759-762

  [5] Haenisch B, Hiemke C, Bönisch H. Inhibitory potencies of trimipramine and its main metabolites at human monoamine and organic cation transporters. Psychopharmacology (Berl). 2011;217(2):289-295

  [6] Lapierre YD. A review of trimipramine. 30 years of clinical use. Drugs. 1989;38 Suppl 1:17-50

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