Klomipramin
Klomipramin (Anafranil) je triciklični antidepresiv (TCA). On je razvijen tokom 1960-tih i od tog vremena je u kliničkoj upotrebi širom sveta.[2][3][4][5]
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| IUPAC ime | |
|---|---|
3-(3-hloro-10,11-dihidro-5H-dibenzo[b,f]azepin-5-il)-N,N-dimetilpropan-1-amin | |
| Klinički podaci | |
| Prodajno ime | Anafranil |
| Drugs.com | Monografija |
| MedlinePlus | a697002 |
| Kategorija trudnoće |
|
| Način primene | Oralno, IM, IV |
| Pravni status | |
| Pravni status |
|
| Farmakokinetički podaci | |
| Bioraspoloživost | Oralno ~50% |
| Metabolizam | Hepatički |
| Poluvreme eliminacije | Klomipramin ~35 sata Desmetilklomipramin (glavni aktivni metabolit) ~50 sata |
| Izlučivanje | Renalno |
| Identifikatori | |
| CAS broj | 303-49-1  |
| ATC kod | N06AA04 (WHO) |
| PubChem | CID 2801 |
| IUPHAR/BPS | 2398 |
| DrugBank | DB01242 |
| ChemSpider | 2699 |
| UNII | NUV44L116D |
| KEGG | D07727 |
| ChEBI | CHEBI:47780 |
| ChEMBL | CHEMBL415 |
| Hemijski podaci | |
| Formula | C19H23ClN2 |
| Molarna masa | 314,9 g/mol |
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Farmakologija уреди
Klomipramin je blokator sledećih transportera:[6]
- Serotoninski transporter (SERT) (Ki = 0.14 nM)
- Norepinefrinski transporter (NET) (Ki = 54 nM)
- Dopaminski transporter (DAT) (Ki = 3,020 nM)
- Glicinski transporter (GlyT/LeuT)
On je antagonist/inverzni agonist sledećih receptora:[6][7][8][9]
- 5-HT2A receptor (Ki = 36 nM)
- 5-HT2C receptor (Ki = 65 nM)
- 5-HT3 receptor (Ki = 85 nM)
- 5-HT6 receptor (Ki = 54 nM)
- 5-HT7 receptor (Ki = 127 nM)
- α1-adrenergički receptor (Ki = 3.2 nM)
- α2-adrenergički receptor (Ki = 525 nM)
- H1 receptor (Ki = 31 nM)
- mACh receptors (Ki = 37 nM)
Aktivni metabolit klomipramina, desmetilklomipramin ispoljava sledeći afinitet:
- Norepinefrinski transporter (NET) (Ki = <1 nM)[10]
Vidi još уреди
Reference уреди
- ^ DailyMed: About DailyMed
- ^ Lemke, T.L., Williams, D.A., Roche, V.T., & Zito, S.W., 2012. Foye's Principles of Medicinal Chemistry. 7th ed. Baltimore, MD: Lippincott Williams & Wilkins, p. 605.
- ^ Healy, D. (2004). Let them eat Prozac: The unhealthy relationship between the pharmaceutical industry and depression. New York: New York University Press, p. 23.
- ^ Beaumont, G., & Healy, D. (1993). The place of clomipramine in the development of psychopharmacology. Journal of Psychopharmacology, 7, 383–393.
- ^ Pichot, P. (1996). The discovery of chlorpromazine and the place of psychopharmacology in the history of psychiatry. The Psychopharmacologists (Vol. 1, pp. 1–21). London, England: Chapman & Hall.
- ^ а б Millan MJ; Gobert A; Lejeune F; et al. (2001). „S33005, a novel ligand at both serotonin and norepinephrine transporters: I. Receptor binding, electrophysiological, and neurochemical profile in comparison with venlafaxine, reboxetine, citalopram, and clomipramine”. The Journal of Pharmacology and Experimental Therapeutics. 298 (2): 565—80. PMID 11454918.[мртва веза]
- ^ Monsma FJ, Shen Y, Ward RP, Hamblin MW, Sibley DR (1993). „Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs”. Molecular Pharmacology. 43 (3): 320—7. PMID 7680751.[мртва веза]
- ^ Ruat M; Traiffort E; Leurs R; et al. (1993). „Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation”. Proceedings of the National Academy of Sciences of the United States of America. 90 (18): 8547—51. PMC 47394
. PMID 8397408. doi:10.1073/pnas.90.18.8547.
- ^ Toll L; Berzetei-Gurske IP; Polgar WE; et al. (1998). „Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications”. NIDA Research Monograph. 178: 440—66. PMID 9686407.
- ^ P K Gillman (2007). „Tricyclic antidepressant pharmacology and therapeutic drug interactions updated”. Br J Pharmacol. 151 (6): 737—748. PMC 2014120 . PMID 17471183. doi:10.1038/sj.bjp.0707253.
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