生物活性

• 描述Duloxetine hydrochloride is a serotonin-norepinephrine reuptake inhibitor (SNRI), used for treatment of major depressive disorder and generalized anxiety disorder (GAD). Duloxetine exhibited moderate anticonvulsive activity with an ED50 (median effective dose) of 48.21 mg/kg in the maximal electroshock test in mice.Single administration of duloxetine (6.25-25 mg/kg) significantly increased the anticonvulsant effects of valproate, carbamazepine, and oxcarbazepine in the maximal electroshock test^[3]. 30 mg/kg of duloxetine could significantly inhibit the hyperexcitability of spinal wide dynamic range (WDR) cells. Duloxetine may have an effective protective action against oxaliplatin-induced neuropathic pain and spinal hyperexcitability, which is mediated by spinal α₁-adrenergic receptors^[4]. Duloxetine can attenuate DR (Diabetic retinopathy) via the anti-inflammatory and the anti-oxidative properties as well as modulating the angiogenic and the neurotrophic factors expressions^[5]. In vivo experiments with a mouse model of prurigo-like inflammation showed that duloxetine hydrochloride ameliorated not only scratching behaviours, but also skin inflammation. Duloxetine hydrochloride appears to be useful for treating prurigo via modulating itch signals and immune responses^[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
  NCT00960986	Major Depressive Disorder (MDD... more >>) Collapse <<	Phase 4	Completed	-	Korea, Republic of ... more >> For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Cheong Ju-City, Korea, Republic of, 361-711 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Goyang-Si, Korea, Republic of, 410-719 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Seongnam-Si, Korea, Republic of, 463-707 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Seoul, Korea, Republic of, 134-791 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Sungnam-Si, Korea, Republic of, 463-712 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Suwon-City, Korea, Republic of, 442-721 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Yangsan, Korea, Republic of, 626-770 Collapse <<
  NCT00296699	Atypical Depression	Phase 4	Completed	-	United States, New York ... more >> Depression Evaluation Service - New York State Psychiatric Institute New York, New York, United States, 10032 Collapse <<
  NCT01127490	Fibromyalgia	Not Applicable	Unknown	December 2012	United States, New York ... more >> Neurosciences Institute, Albany Medical College Recruiting Albany, New York, United States, 12208 Principal Investigator: Charles Argoff, MD Collapse <<

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• 参考文献

• [1] Alarfaj NA, Ammar RA, El-Tohamy MF. Disposable screen-printed sensors for determination of duloxetine hydrochloride. Chem Cent J. 2012 Jan 21;6:6.

  [2] Wong DT, Robertson DW, et al. LY227942, an inhibitor of serotonin and norepinephrine uptake: biochemical pharmacology of a potential antidepressant drug. Life Sci. 1988;43(24):2049-57.

  [3] Wu Y, Huang Y, Song M, Zhang Z, Liang Z, Deng X. Anticonvulsive activity of duloxetine: A new choice for the epileptic patients with depression. Pak J Pharm Sci. 2019 May;32(3):997-1003

  [4] Kim W, Chung Y, Choi S, Min BI, Kim SK. Duloxetine Protects against Oxaliplatin-Induced Neuropathic Pain and Spinal Neuron Hyperexcitability in Rodents. Int J Mol Sci. 2017 Dec 5;18(12):2626

  [5] Bahr HI, Abdelghany AA, Galhom RA, Barakat BM, Arafa EA, Fawzy MS. Duloxetine protects against experimental diabetic retinopathy in mice through retinal GFAP downregulation and modulation of neurotrophic factors. Exp Eye Res. 2019 Sep;186:107742

  [6] Hashimoto T, Satoh T, Yokozeki H. Prurigo successfully treated with duloxetine hydrochloride. Australas J Dermatol. 2019 Aug;60(3):237-239

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