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Amoksapin Садржај Farmakologija Reference Vidi još Spoljašnje veze Мени за навигацијуMonografijaa68220214028-44-5WHO2170201DB005432085R63VQ857OTD00228CHEBI:2675CHEMBL11136764165„Pharmacological profile of antidepressants and related compounds at human monoamine transporters”953782110.1016/S0014-2999(97)01393-9„Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2c receptor”887602310.1007/BF02246453„Further evidence that 5-HT-induced relaxation of pig pulmonary artery is mediated by endothelial 5-HT2B receptors”15721011082180010.1038/sj.bjp.07033411666997„Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors”7908055„Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro”6086881„Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist”1613569910.1124/jpet.105.0921551966571„Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist”1594703610.1124/jpet.105.087965уууууу

Инхибитори преузимања норепинефринаИнхибитори преузимања серотонинаПиперазиниЛечење биполарног поремећајаДибензоксазепиниХлороарени5-ХТ7 антагонисти


tetraciklični antidepresivdibenzoksazepinsketriciklični antidepresivLoksapinainhibitor preuzimanjaserotoninanorepinefrina5-HT2A5-HT2B5-HT2C5-HT35-HT65-HT7D2α1-adrenergičkiD3D4H1 receptorafinitetomantagonistinverzni agonistdopaminski transporter5-HT1A5-HT1BD1α2-adrenergičkiH4mAChGABAA receptorβ-adrenergičke receptorealosternabenzodiazepinska mestaMPSOPSImeprdsrdodbpasspecspvoprocN5A5B5C6A6B6DAzaperonBenperidolBromperidolDroperidolFluanizonHaloperidolLenperonMoperonPipamperonSpiperonTimiperonTrifluperidolKlopimozidFluspirilenPenfluridolPimozidAcepromazinAcetofenazinButaperazinKarfenazinHloracizinHlorproetazinHlorpromazinCijamemazinDiksirazinFluacizinFlufenazinLevomepromazin/MetotrimeprazinMezoridazinPerazinPericijazinPerfenazinPiperacetazinPipotiazinProhlorperazinPromazinPrometazinPropiomazinSulforidazinTietilperazinTiopropazatTioproperazinTioridazinTrifluoperazinTriflupromazinHlorprotiksenKlopentiksolFlupentiksolTiotiksenZuklopentiksolButaklamolFluotracenLoksapinTrimipraminCinuperonMelperonSetoperonIloperidonOkaperidonPaliperidonRisperidonLurasidonePerospironRevospironTiospironZiprasidonAmperozidAripiprazolBifeprunoksBrekspiprazolElopiprazolUmespironAmoksapinAsenapinKarpipraminKlocapraminKlorotepinKlotiapinKlozapinFluperlapinGevotrolinMetitepinMosapraminNDMCOlanzapinPihindonKvetijapinTenilapinZotepinWHO-EMPovučeniKlinička ispitivanjaFaza IIINije dospeo do faze IIIMPSOPSImeprdsrdodbpasspecspvoprocN5A5B5C6A6B6DAkrivastinAlinastinAstemizolAzelastinBamirastinBarmastinBepiastinBepotastinBilastinKabastinenKarebastinKetirizinKlemastinKlemizolKlobenztropinDorastinEbastinEmedastinEpinastinFlezelastinKetotifenLatrepirdinLevokabastinLinetastinLoratadinMapinastinMebhidrolinMizolastinMoksastinNoberastinOktastinOlopatadinPerastinPiklopastinRokastinRupatadinSetastinTalastinTemelastinTerfenadinZepastinDesloratadinFeksofenadinCetirizin‎‎LevocetirizinBelarizinEfletirizinElbanizinFlotrenizinMedrilaminNapaktadinPibaksizinTagorizinTrelnarizinTrenizinVapitadin










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Amoksapin




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Amoksapin (Amokisan, Asendin, Asendis, Defanil, Demoloks, Moksadil) je tetraciklični antidepresiv iz dibenzoksazepinske familije, mada se on često klasifikuje kao sekundarni aminski triciklični antidepresiv. On je N-demetilisani metabolit Loksapina.




Садржај





  • 1 Farmakologija


  • 2 Reference


  • 3 Vidi još


  • 4 Spoljašnje veze




Farmakologija


Amoksapin ispoljava mnoštvo farmakoloških efekata. On je umeren i jak inhibitor preuzimanja serotonina i norepinefrina, respektivno,[2] i vezuje se za 5-HT2A,[3]5-HT2B,[4]5-HT2C,[3]5-HT3,[5]5-HT6,[6]5-HT7,[6]D2,[7]α1-adrenergički,[7]D3[8], D4,[8] i H1 receptor[7] sa promenljivim ali značajnim afinitetom, na njijima deluje kao antagonist (ili inverzni agonist u zavisnosti od receptora) na svim aktivnim mestima. On ima slab i zanemarljiv afinitet za dopaminski transporter i 5-HT1A,[5]5-HT1B,[5]D1,[9]α2-adrenergički,[7]H4,[10]mACh,[7] i GABAA receptor,[9] i nema afiniteta za β-adrenergičke receptore ili za alosterna benzodiazepinska mesta na GABAA receptoru.[9]



Reference




  1. 1,01,1 Kinney JL, Evans RL (1982). „Evaluation of amoxapine”. Clinical Pharmacy. 1 (5): 417—24. PMID 6764165. 


  2. ^ Tatsumi M, Groshan K, Blakely RD, Richelson E (1997). „Pharmacological profile of antidepressants and related compounds at human monoamine transporters”. European Journal of Pharmacology. 340 (2–3): 249—58. PMID 9537821. doi:10.1016/S0014-2999(97)01393-9. 


  3. 3,03,1 Pälvimäki EP; Roth BL; Majasuo H; et al. (1996). „Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2c receptor”. Psychopharmacology. 126 (3): 234—40. PMID 8876023. doi:10.1007/BF02246453. CS1 одржавање: Експлицитна употреба et al. (веза)


  4. ^ Glusa E, Pertz HH (2000). „Further evidence that 5-HT-induced relaxation of pig pulmonary artery is mediated by endothelial 5-HT2B receptors”. British Journal of Pharmacology. 130 (3): 692—8. PMC 1572101 Слободан приступ. PMID 10821800. doi:10.1038/sj.bjp.0703341. 


  5. 5,05,15,2 Gozlan H, Saddiki-Traki F, Merahi N, Laguzzi R, Hamon M (1991). „[Preclinical pharmacology of amoxapine and amitriptyline. Implications of serotoninergic and opiodergic systems in their central effect in rats]”. L'Encéphale (на језику: French). 17 Spec No 3: 415—22. PMID 1666997. CS1 одржавање: Непрепознат језик (веза)


  6. 6,06,1 Roth BL; Craigo SC; Choudhary MS; et al. (1994). „Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors”. The Journal of Pharmacology and Experimental Therapeutics. 268 (3): 1403—10. PMID 7908055. CS1 одржавање: Експлицитна употреба et al. (веза)


  7. 7,07,17,27,37,4 Richelson E, Nelson A (1984). „Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro”. The Journal of Pharmacology and Experimental Therapeutics. 230 (1): 94—102. PMID 6086881. 


  8. 8,08,1 Burstein ES; Ma J; Wong S; et al. (2005). „Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist”. The Journal of Pharmacology and Experimental Therapeutics. 315 (3): 1278—87. PMID 16135699. doi:10.1124/jpet.105.092155. CS1 одржавање: Експлицитна употреба et al. (веза)


  9. 9,09,19,2 Wei HB, Niu XY (1990). „[Comparison of the affinities of amoxapine and loxapine for various receptors in rat brain and the receptor down-regulation after chronic administration]”. Yao Xue Xue Bao = Acta Pharmaceutica Sinica (на језику: Chinese). 25 (12): 881—5. PMID 1966571. CS1 одржавање: Непрепознат језик (веза)


  10. ^ Lim HD, van Rijn RM, Ling P, Bakker RA, Thurmond RL, Leurs R (2005). „Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist”. The Journal of Pharmacology and Experimental Therapeutics. 314 (3): 1310—21. PMID 15947036. doi:10.1124/jpet.105.087965. 



Vidi još


  • Loksapin


Spoljašnje veze




Amoksapin
Amoxapine.svg

IUPAC ime
2-hloro-11-(piperazin-1-il)dibenzo[b,f][1,4]oksazepin
Klinički podaci
Prodajno imeAsendin
Drugs.comMonografija
MedlinePlusa682202
Kategorija trudnoće


  • US: C (Mogući rizik)

Način primeneOralnot
Pravni status
Pravni status


  • US: ℞-only


Farmakokinetički podaci
Bioraspoloživost?
Vezivanje proteina90%[1]
MetabolizamHepatički (citohrom P450)
Poluvreme eliminacije8-10 sata (30 sata za glavne metabolite)[1]
IzlučivanjeRenal

Identifikatori
CAS broj
14028-44-5 ДаY
ATC kod
N06AA17 (WHO)
PubChemCID 2170
IUPHAR/BPS201
DrugBank
DB00543 ДаY
ChemSpider
2085 ДаY
UNII
R63VQ857OT ДаY
KEGG
D00228 ДаY
ChEBI
CHEBI:2675 ДаY
ChEMBL
CHEMBL1113 ДаY
Hemijski podaci
Formula
C17H16ClN3O
Molarna masa313,781 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)