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Asenapin Sinteza References Spoljašnje veze Мени за навигацијуMonografijaa61001565576-45-6WHO163091222300725JKZ19V908OCHEMBL1201756„Schering-Plough Announces Asenapine NDA Accepted for Filing by the U.S. FDA”„FDA Drug Safety Communication: Serious allergic reactions reported with the use of Saphris (asenapine maleate)”U.S. Patent 4.145.434Saphris websiteOrganon websiteOrganon Continues With The Development Of Asenapine For Schizophrenia And Acute Mania Associated With Bipolar I Disorderууууу

Атипични антипсихотициМодулатори рецептораОксепиниХлороарениПиролизидини5-ХТ6 антагонисти


atipični antipsihotikšizofrenijebipolar poremećajfazu IIIAkzo Nobelakliničkim ispitivanjimaFDA2009natrijumamonijakuAzaperonBenperidolBromperidolDroperidolFluanizonHaloperidolLenperonMoperonPipamperonSpiperonTimiperonTrifluperidolKlopimozidFluspirilenPenfluridolPimozidAcepromazinAcetofenazinButaperazinKarfenazinHloracizinHlorproetazinHlorpromazinCijamemazinDiksirazinFluacizinFlufenazinLevomepromazin/MetotrimeprazinMezoridazinPerazinPericijazinPerfenazinPiperacetazinPipotiazinProhlorperazinPromazinPrometazinPropiomazinSulforidazinTietilperazinTiopropazatTioproperazinTioridazinTrifluoperazinTriflupromazinHlorprotiksenKlopentiksolFlupentiksolTiotiksenZuklopentiksolButaklamolFluotracenLoksapinTrimipraminCinuperonMelperonSetoperonIloperidonOkaperidonPaliperidonRisperidonLurasidonePerospironRevospironTiospironZiprasidonAmperozidAripiprazolBifeprunoksBrekspiprazolElopiprazolUmespironAmoksapinAsenapinKarpipraminKlocapraminKlorotepinKlotiapinKlozapinFluperlapinGevotrolinMetitepinMosapraminNDMCOlanzapinPihindonKvetijapinTenilapinZotepinWHO-EMPovučeniKlinička ispitivanjaFaza IIINije dospeo do faze IIIMPSOPSImeprdsrdodbpasspecspvoprocN5A5B5C6A6B6DAkrivastinAlinastinAstemizolAzelastinBamirastinBarmastinBepiastinBepotastinBilastinKabastinenKarebastinKetirizinKlemastinKlemizolKlobenztropinDorastinEbastinEmedastinEpinastinFlezelastinKetotifenLatrepirdinLevokabastinLinetastinLoratadinMapinastinMebhidrolinMizolastinMoksastinNoberastinOktastinOlopatadinPerastinPiklopastinRokastinRupatadinSetastinTalastinTemelastinTerfenadinZepastinDesloratadinFeksofenadinCetirizin‎‎LevocetirizinBelarizinEfletirizinElbanizinFlotrenizinMedrilaminNapaktadinPibaksizinTagorizinTrelnarizinTrenizinVapitadin










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Asenapin




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Asenapin (Safris, Sikrest) je atipični antipsihotik koji je razvijen za tretman šizofrenije i akutne manije vezane za bipolar poremećaj. Lek je ušao u fazu III kliničkih ispitivanja do je Organon još bio deo Akzo Nobela.[1] Preliminarni podaci indiciraju da asenapin proizvodi minimalne antiholinergičke i kardiovaskularne nuspojave, kao i minimalno uvećanje telesne težine. Preko 3000 pacijenata je učestvovalo u kliničkim ispitivanjima, i FDA je odobrila lek 2009.[2][3]



Sinteza


Jedan od mogućih sintetičkih puteva je[4]


Asenapine scheme.png

U reducionom koraku se koristi natrijum u tečnom amonijaku.



References




  1. ^ „Bipolar Disorder”. Clinical Trials Update. Genetic Engineering & Biotechnology News. 15. 6. 2007. стр. 52,55.  |access-date= захтева |url= (помоћ)


  2. ^ „Schering-Plough Announces Asenapine NDA Accepted for Filing by the U.S. FDA” (Саопштење). Schering-Plough. 26. 11. 2007. Приступљено 29. 12. 2008. 


  3. ^ „FDA Drug Safety Communication: Serious allergic reactions reported with the use of Saphris (asenapine maleate)”. 


  4. ^ J. van der Burg, U.S. Patent 4.145.434.



Spoljašnje veze



  • Saphris website

  • Organon website

  • Organon Continues With The Development Of Asenapine For Schizophrenia And Acute Mania Associated With Bipolar I Disorder


Asenapin
Skeletal formula
Ball-and-stick model

IUPAC ime
(3aRS,12bRS)-rel-5-hloro-2,3,3a,12b-tetrahidro-
2-metil-1H-dibenz[2,3:6,7]oksepino[4,5-c]pirol
Klinički podaci
Drugs.comMonografija
MedlinePlusa610015
Kategorija trudnoće


  • US: C (Mogući rizik)

Način primenesablingualno
Pravni status
Pravni status

  • ℞ (Prescription only)


Farmakokinetički podaci
Bioraspoloživost35% sablingualno
Vezivanje proteina95%
Metabolizamhepatički
Poluvreme eliminacije24 sata
Izlučivanje50% urin, 40% izmet

Identifikatori
CAS broj
65576-45-6 ДаY
ATC kod
N05AH05 (WHO)
PubChemCID 163091
IUPHAR/BPS22
ChemSpider
2300725 ДаY
UNII
JKZ19V908O ДаY
ChEMBL
CHEMBL1201756 ДаY
Hemijski podaci
Formula
C17H16ClNO
Molarna masa285,77 g/mol




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Кастелфранко ди Сопра Становништво Референце Спољашње везе Мени за навигацију43°37′18″ СГШ; 11°33′32″ ИГД / 43.62156° СГШ; 11.55885° ИГД / 43.62156; 11.5588543°37′18″ СГШ; 11°33′32″ ИГД / 43.62156° СГШ; 11.55885° ИГД / 43.62156; 11.558853179688„The GeoNames geographical database”„Istituto Nazionale di Statistica”проширитиууWorldCat156923403n850174324558639-1cb14643287r(подаци)

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