賽他發定

賽他發定
法律規範狀態
法律規範	美：Investigational New Drug;
識別資訊
	IUPAC命名法 (1R,5S)-1-naphthalen-2-yl-3-azabicyclo[3.1.0]hexane; ;
CAS號	924012-43-1
PubChem CID	16095349;
ChemSpider	17253639;
UNII	D2A6T4UH9C;
KEGG	D10697 ;
CompTox Dashboard（英語：CompTox Chemicals Dashboard） (EPA)	DTXSID201045788 ;
化學資訊
化學式	C15H15N
摩爾質量	209.29 g·mol−1
3D模型（JSmol（英語：JSmol））	交互式圖像;
	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;

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、多巴胺和血清素的再攝取。^[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]

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

^ ^1.0 ^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].
^ 3-Neurotransmitters, 1-Molecule: Optimized Ratios. Neurovance.
^ 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）.
^ 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].
^ EUTHYMICS BIOSCIENCE, INC. PRESENTS DATA THAT SUPPORT ADVANCING EB-1020 INTO CLINICAL TRIALS FOR ADULT ADHD (PDF). Neurovance. December 7, 2011 [14 January 2018].
^ Otsuka Pharmaceutical to Acquire Neurovance, Inc.. Otsuka. [14 January 2018].
^ 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.

外部連結

Centanafadine - AdisInsight

這是一篇作用於神經系統的藥品小作品。您可以透過編輯或修訂擴充其內容。

[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].

[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.

[euthymics-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].

[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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法律規範狀態

法律規範	美：Investigational New Drug
識別資訊
IUPAC命名法 (1R,5S)-1-naphthalen-2-yl-3-azabicyclo[3.1.0]hexane
CAS號	924012-43-1
PubChem CID	16095349
ChemSpider	17253639
UNII	D2A6T4UH9C
KEGG	D10697^Y
CompTox Dashboard（英語：CompTox Chemicals Dashboard） (EPA)	DTXSID201045788
化學資訊
化學式	C₁₅H₁₅N
摩爾質量	209.29 g·mol⁻¹
3D模型（JSmol（英語：JSmol））	交互式圖像
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