賽他發定

化合物

賽他發定INN:centanafadine;開發代號:EB-1020)是一種血清素-去甲腎上腺素-多巴胺再攝取抑制劑(也叫三重再攝取抑制劑),在Euthymics Bioscience收購DOV製藥英語DOV Pharmaceutical後開始開發。它被開發用於治療注意力缺陷多動障礙,並分別以1:6:14的比例抑制去甲腎上腺素多巴胺血清素的再攝取。[1][2][3][4]2011年,Euthymics Bioscience將他們的賽他發定開發業務剝離給了一家名為Neurovance的新公司。[5][6]2017年3月,大冢製藥收購了Neurovance和賽他發定的專利。[7]截至2018年1月,大冢的研發管線顯示其正在進行II期和III期臨床試驗,以應對多種不同的醫療狀況。[8][9][10]

賽他發定
法律規範狀態
法律規範
  • Investigational New Drug
識別資訊
  • (1R,5S)-1-naphthalen-2-yl-3-azabicyclo[3.1.0]hexane
CAS號924012-43-1
PubChem CID
ChemSpider
UNII
KEGG
CompTox Dashboard英語CompTox Chemicals Dashboard (EPA)
化學資訊
化學式C15H15N
摩爾質量209.29 g·mol−1
3D模型(JSmol英語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]
位點 IC50 (nM) 作用 參考
SERT 83 nM 阻滯劑 [1]
NET 6 nM 阻滯劑 [1]
DAT 38 nM 阻滯劑 [1]

參見

參考資料

  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]. (原始內容 (PDF)存檔於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. 

外部連結