赛他发定

化合物

赛他发定INN:centanafadine;开发代号:EB-1020)是一种血清素-去甲肾上腺素-多巴胺再摄取抑制剂(也叫三重再摄取抑制剂),在Euthymics Bioscience收购DOV制药英语DOV Pharmaceutical后开始开发。它被开发用于治疗注意力缺陷多动障碍,并分别以1:6:14的比例抑制去甲肾上腺素多巴胺血清素的再摄取。[1][2][3][4]2011年,Euthymics Bioscience将他们的赛他发定开发业务剥离给了一家名为Neurovance的新公司。[5][6]2017年3月,大冢制药收购了Neurovance和赛他发定的专利。[7]截至2018年1月,大冢的研发管线显示其正在进行II期和III期临床试验,以应对多种不同的医疗状况。[8][9][10]

赛他发定
法律規範狀態
法律規範
  • Investigational New Drug
识别信息
  • (1R,5S)-1-naphthalen-2-yl-3-azabicyclo[3.1.0]hexane
CAS号924012-43-1
PubChem CID
ChemSpider
UNII
KEGG
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
化学信息
化学式C15H15N
摩尔质量209.29 g·mol−1
3D模型(JSmol英语JSmol
  • C1=C(C=CC2=CC=CC=C12)[C@@]34C[C@@H]3CNC4
  • InChI=1S/C15H15N/c1-2-4-12-7-13(6-5-11(12)3-1)15-8-14(15)9-16-10-15/h1-7,14,16H,8-10H2/t14-,15+/m1/s1
  • Key:HKHCSWPSUSWGLI-CABCVRRESA-N
Centanafadine [1]
位点 IC50 (nM) 作用 参考
SERT 83 nM 阻滞剂 [1]
NET 6 nM 阻滞剂 [1]
DAT 38 nM 阻滞剂 [1]

参见

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参考资料

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  1. ^ 1.0 1.1 1.2 1.3 1.4 Neurovance's EB-1020 SR for Adult ADHD Shows Stimulant-Like Efficacy and Good Tolerability in Phase 2a Trial (PDF). Neurovance. [14 January 2018]. 
  2. ^ 3-Neurotransmitters, 1-Molecule: Optimized Ratios. Neurovance. 
  3. ^ EB-1020, a Non-Stimulant Norepinephrine and Dopamine - Preferring Reuptake Inhibitor for the Treatment of Adult ADHD (PDF). Neurovance. [2015-11-14]. (原始内容 (PDF)存档于2015-11-17). 
  4. ^ Bymaster FP, Golembiowska K, Kowalska M, Choi YK, Tarazi FI. Pharmacological characterization of the norepinephrine and dopamine reuptake inhibitor EB-1020: implications for treatment of attention-deficit hyperactivity disorder. Synapse. June 2012, 66 (6): 522–32. PMID 22298359. S2CID 38850652. doi:10.1002/syn.21538. 
  5. ^ Euthymics. Ethismos Research Inc. [14 January 2018]. 
  6. ^ EUTHYMICS BIOSCIENCE, INC. PRESENTS DATA THAT SUPPORT ADVANCING EB-1020 INTO CLINICAL TRIALS FOR ADULT ADHD (PDF). Neurovance. December 7, 2011 [14 January 2018]. 
  7. ^ Otsuka Pharmaceutical to Acquire Neurovance, Inc.. Otsuka. [14 January 2018]. 
  8. ^ Otsuka U.S. Research & Development Programs. Otsuka U.S. Otsuka. [14 January 2018]. [永久失效連結]
  9. ^ Otsuka Pharmaceutical Development & Commercialization, Inc. A Phase 3, Randomized, Double-blind, Multicenter, Placebo-controlled, Parallel-group Trial Evaluating the Efficacy, Safety, and Tolerability of Centanafadine Sustained-release Tablets in Adults With Attention-deficit/Hyperactivity Disorder. 2021-09-17. 
  10. ^ Gunduz-Bruce, Handan. SAGE-217 in major depressive disorder: a multicenter, randomized, double-blind, Phase 2 placebo-controlled trial. 2018-09-26 [2023-06-26]. S2CID 266120058. doi:10.26226/morressier.5b68175eb56e9b005965c44b. 

外部链接

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