赛他发定

赛他发定
法律規範狀態
法律規範	美：Investigational New Drug;
识别信息
	IUPAC命名法 (1R,5S)-1-naphthalen-2-yl-3-azabicyclo[3.1.0]hexane; ;
CAS号	924012-43-1
PubChem CID	16095349;
ChemSpider	17253639;
UNII	D2A6T4UH9C;
KEGG	D10697 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID201045788 ;
化学信息
化学式	C15H15N
摩尔质量	209.29 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES C1=C(C=CC2=CC=CC=C12)[C@@]34C[C@@H]3CNC4;
	InChI 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]

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、多巴胺和血清素的再摄取。^[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]

参见

参考资料

^ ^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]. （原始内容存档 (PDF)于2021-11-04）.
^ 3-Neurotransmitters, 1-Molecule: Optimized Ratios. Neurovance. [2024-06-03]. （原始内容存档于2022-08-09）.
^ 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）.
^ 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.
^ Euthymics. Ethismos Research Inc. [14 January 2018]. （原始内容存档于2024-09-28）.
^ EUTHYMICS BIOSCIENCE, INC. PRESENTS DATA THAT SUPPORT ADVANCING EB-1020 INTO CLINICAL TRIALS FOR ADULT ADHD (PDF). Neurovance. December 7, 2011 [14 January 2018]. （原始内容存档 (PDF)于2023-05-29）.
^ Otsuka Pharmaceutical to Acquire Neurovance, Inc.. Otsuka. [14 January 2018]. （原始内容存档于2024-06-03）.
^ Otsuka U.S. Research & Development Programs. Otsuka U.S. Otsuka. [14 January 2018]. ^{[永久失效連結]}
^ 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.
^ 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

Centanafadine - AdisInsight （页面存档备份，存于互联网档案馆）

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[nM-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]. （原始内容存档 (PDF)于2021-11-04）.

[2] 3-Neurotransmitters, 1-Molecule: Optimized Ratios. Neurovance. [2024-06-03]. （原始内容存档于2022-08-09）.

[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.

[euthymics-5] Euthymics. Ethismos Research Inc. [14 January 2018]. （原始内容存档于2024-09-28）.

[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]. （原始内容存档 (PDF)于2023-05-29）.

[7] Otsuka Pharmaceutical to Acquire Neurovance, Inc.. Otsuka. [14 January 2018]. （原始内容存档于2024-06-03）.

[Otsuka-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.

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