Amoksapin
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.
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| IUPAC ime | |
|---|---|
2-hloro-11-(piperazin-1-il)dibenzo[b,f][1,4]oksazepin | |
| Klinički podaci | |
| Prodajno ime | Asendin |
| Drugs.com | Monografija |
| MedlinePlus | a682202 |
| Kategorija trudnoće |
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| Način primene | Oralnot |
| Pravni status | |
| Pravni status |
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| Farmakokinetički podaci | |
| Bioraspoloživost | ? |
| Vezivanje proteina | 90%[1] |
| Metabolizam | Hepatički (citohrom P450) |
| Poluvreme eliminacije | 8-10 sata (30 sata za glavne metabolite)[1] |
| Izlučivanje | Renal |
| Identifikatori | |
| CAS broj | 14028-44-5  |
| ATC kod | N06AA17 (WHO) |
| PubChem | CID 2170 |
| IUPHAR/BPS | 201 |
| DrugBank | DB00543 |
| ChemSpider | 2085 |
| UNII | R63VQ857OT |
| KEGG | D00228 |
| ChEBI | CHEBI:2675 |
| ChEMBL | CHEMBL1113 |
| Hemijski podaci | |
| Formula | C17H16ClN3O |
| Molarna masa | 313,781 g/mol |
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Farmakologija уреди
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 уреди
- ^ а б Kinney JL, Evans RL (1982). „Evaluation of amoxapine”. Clinical Pharmacy. 1 (5): 417—24. PMID 6764165.
- ^ 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.
- ^ а б 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.
- ^ 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
. PMID 10821800. doi:10.1038/sj.bjp.0703341.
- ^ а б в 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.
- ^ а б 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.
- ^ а б в г д 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. Архивирано из оригинала 28. 08. 2021. г. Приступљено 19. 11. 2012.
- ^ а б 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.
- ^ а б в 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.
- ^ 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. Архивирано из оригинала 13. 12. 2019. г. Приступљено 19. 11. 2012.
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