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词条 Dasotraline
释义

  1. Side Effects

  2. See also

  3. References

  4. Further reading

{{Drugbox
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| image = Dasotraline.svg
| width = 200
| IUPAC_name = (1R,4S)-4-(3,4-Dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine
| tradename =
| bioavailability =
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| ATC_prefix =
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| C=16 | H=15 | Cl=2 | N=1
| CAS_number = 675126-05-3
| CAS_number_Ref = {{cascite|correct|CAS}}
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 4D28EY0L5T
| PubChem = 9947999
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| ChEMBL = 3301595
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| ChemSpiderID = 8123611
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| KEGG = D10700
| smiles = C1C[C@H](C2=CC=CC=C2[C@@H]1C3=CC(=C(C=C3)Cl)Cl)N
| StdInChI = 1S/C16H15Cl2N/c17-14-7-5-10(9-15(14)18)11-6-8-16(19)13-4-2-1-3-12(11)13/h1-5,7,9,11,16H,6,8,19H2/t11-,16+/m0/s1
| StdInChIKey = SRPXSILJHWNFMK-MEDUHNTESA-N
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Dasotraline (INN;[1] former developmental code name SEP-225,289) is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI) that is under development by Sunovion for clinical use.[2][3][4][5] In 2017, the U.S. Food and Drug Administration accepted Sunovion's New Drug Application for review for the treatment of ADHD;[6] the NDA for dasotraline is expected to be decided by the end of August 2018.[7] The drug is no longer being developed for major depressive disorder (MDD), but is still under investigation for the treatment of attention-deficit hyperactivity disorder (ADHD) and eating disorders.[8][9] Structurally, dasotraline is a stereoisomer of desmethylsertraline, which is an active metabolite of the marketed selective serotonin reuptake inhibitor (SSRI) antidepressant sertraline (Zoloft) and an SNDRI similarly.

Side Effects

In phase I trials for ADHD, test subjects reported the following side effects:[10][11]

  • Loss of appetite
  • Dehydration
  • Dry mouth
  • Nausea
  • Insomnia
  • Anxiety
  • Panic attacks
  • Headaches

See also

  • Centanafadine
  • Indatraline
  • Lometraline
  • Tametraline

References

1. ^{{cite journal |title=International Nonproprietary Names for Pharmaceutical Substances (INN) |journal=WHO Drug Information |volume=27 |issue=4 |year=2013 |url=http://www.who.int/medicines/publications/druginformation/PL_110.pdf |publisher=WHO |accessdate=4 November 2014}}
2. ^{{cite journal |last1=Chen |first1=Zhengming |last2=Skolnick |first2=Phil |title=Triple uptake inhibitors: therapeutic potential in depression and beyond |journal=Expert Opinion on Investigational Drugs |volume=16 |issue=9 |pages=1365–77 |year=2007 |pmid=17714023 |doi=10.1517/13543784.16.9.1365 }}
3. ^{{cite journal |last1=DeLorenzo |first1=C. |last2=Lichenstein |first2=S. |last3=Schaefer |first3=K. |last4=Dunn |first4=J. |last5=Marshall |first5=R. |last6=Organisak |first6=L. |last7=Kharidia |first7=J. |last8=Robertson |first8=B. |last9=Mann |first9=J. J. |last10=Parsey |first10=R. V. |title=SEP-225289 Serotonin and Dopamine Transporter Occupancy: A PET Study |journal=Journal of Nuclear Medicine |volume=52 |issue=7 |pages=1150–5 |year=2011 |pmid=21680689 |pmc=3856248 |doi=10.2967/jnumed.110.084525 }}
4. ^{{cite journal |last1=Ziegler |first1=L. |last2=Küffer |first2=G. |last3=Euler |first3=E. |last4=Wilhelm |first4=K. |title=Arthrographische Darstellung von Ganglien im Handbereich |trans-title=Arthrographic imaging of ganglions of the hand |language=German |journal=RöFo |volume=153 |issue=2 |pages=143–6 |year=1990 |pmid=2168068 |doi=10.1055/s-2008-1033352 }}
5. ^{{cite journal |last1=Guiard |first1=B. |last2=Chenu |first2=F. |last3=El Mansari |first3=M. |last4=Blier |first4=P. |title=P.1.c.059 Electrophysiological properties of the triple reuptake inhibitor SEP 225289 on monoaminergic neurons |journal=European Neuropsychopharmacology |volume=19 |year=2009 |pages=S285 |doi=10.1016/S0924-977X(09)70419-5 }}
6. ^{{cite press release |author= |title=Sunovion Announces FDA Acceptance for Review of New Drug Application for Dasotraline for the Treatment of ADHD |url=http://news.sunovion.com/press-release/sunovion-announces-fda-acceptance-review-new-drug-application-dasotraline-treatment |location=Marlborough, Massachusetts |publisher=Sunovion |agency=Business Wire |date=November 10, 2017 |access-date=2018-05-01}}
7. ^{{cite web|title=Pipeline Report: Brand Drugs|url=https://www.welldynerx.com/content/uploads/2018/02/PipelineReport-Brand-Drugs.pdf|publisher=Welldyne|accessdate=1 May 2018|pages=1, 4|format=PDF|date=February 2018}}
8. ^{{ClinicalTrialsGov|NCT02276209|Dasotraline Adult ADHD Study}}
9. ^http://adisinsight.springer.com/drugs/800023450{{full citation needed|date=September 2018}}
10. ^{{cite journal |last1=Koblan |first1=Kenneth S |last2=Hopkins |first2=Seth C |last3=Sarma |first3=Kaushik |last4=Jin |first4=Fengbin |last5=Goldman |first5=Robert |last6=Kollins |first6=Scott H |last7=Loebel |first7=Antony |title=Dasotraline for the Treatment of Attention-Deficit/Hyperactivity Disorder: A Randomized, Double-Blind, Placebo-Controlled, Proof-of-Concept Trial in Adults |journal=Neuropsychopharmacology |volume=40 |issue=12 |pages=2745–52 |year=2015 |pmid=25948101 |doi=10.1038/npp.2015.124 |pmc=4864650}}
11. ^http://www.additudemag.com/adhdblogs/19/11101.html{{full citation needed|date=September 2018}}

Further reading

Liming Shao Patent
  • {{ cite patent | country = US | number = 2007203111 | status = application | title = Cycloalkylamines as monoamine reuptake inhibitors | pubdate = 2007-08-30 | inventor =Shao L, Wang F, Malcolm SC, Hewitt MC, Bush LR, Ma J, Varney MA, Campbell U, Engel SR, Hardy LW, Koch P, Campbell JE | assign1 = Sepracor Inc. | class = }}
Asymmetry Patent
  • {{ cite patent | country = US | number = 7129378 | status = patent | title = Method of preparing amine stereoisomers | pubdate = 2005-07-28 | inventor = Han X, Krishnamurthy D, Senanayake CH, Lu Z-H | assign1 = Apsinterm LLC | class = }}
{{Monoamine reuptake inhibitors}}

3 : Serotonin-norepinephrine-dopamine reuptake inhibitors|Chloroarenes|Amines

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