Klomipramin

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Klomipramin
(IUPAC) ime
3-(3-hloro-10,11-dihidro-5H-dibenzo[b,f]azepin-5-il)-N,N-dimetilpropan-1-amin
Klinički podaci
Robne marke Anafranil
AHFS/Drugs.com Monografija
MedlinePlus a697002
Identifikatori
CAS broj 303-49-1
ATC kod N06AA04
PubChem[1][2] 2801
DrugBank DB01242
ChemSpider[3] 2699
UNII NUV44L116D YesY
KEGG[4] D07727 YesY
ChEBI CHEBI:47780 YesY
ChEMBL[5] CHEMBL415 YesY
Hemijski podaci
Formula C19H23ClN2 
Mol. masa 314,9 g/mol
SMILES eMolekuli & PubHem
Farmakokinetički podaci
Bioraspoloživost Oralno ~50%
Metabolizam Hepatički
Poluvreme eliminacije Klomipramin ~35 sata
Desmetilklomipramin (glavni aktivni metabolit) ~50 sata
Izlučivanje Renalno
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status Prescription only
Način primene Oralno, IM, IV

Klomipramin (Anafranil) je triciklični antidepresiv (TCA). On je razvijen tokom 1960-tih i od tog vremena je u kliničkoj upotrebi širom sveta.[6][7][8][9]

Farmakologija[uredi - уреди | uredi izvor]

Klomipramin je blokator sledećih transportera:[10]

On je antagonist/inverzni agonist sledećih receptora:[10][11][12][13]

Aktivni metabolit klomipramina, desmetilklomipramin ispoljava sledeći afinitet:

Reference[uredi - уреди | uredi izvor]

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). "PubChem as a public resource for drug discovery.". Drug Discov Today 15 (23-24): 1052–7. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). "Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities". Annual Reports in Computational Chemistry 4: 217–241. doi:10.1016/S1574-1400(08)00012-1. 
  3. Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). "Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining". J Cheminform 2 (1): 3. PMID 20331846. doi:10.1186/1758-2946-2-3.  edit
  4. Joanne Wixon, Douglas Kell (2000). "Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG". Yeast 17 (1): 48–55. doi:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H. 
  5. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). "ChEMBL: a large-scale bioactivity database for drug discovery". Nucleic Acids Res 40 (Database issue): D1100–7. PMID 21948594. doi:10.1093/nar/gkr777.  edit
  6. 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.
  7. Healy, D. (2004). Let them eat Prozac: The unhealthy relationship between the pharmaceutical industry and depression. New York: New York University Press, p. 23.
  8. Beaumont, G., & Healy, D. (1993). The place of clomipramine in the development of psychopharmacology. Journal of Psychopharmacology, 7, 383–393.
  9. 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.
  10. 10,0 10,1 Millan MJ, Gobert A, Lejeune F et al. (August 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. 
  11. Monsma FJ, Shen Y, Ward RP, Hamblin MW, Sibley DR (March 1993). "Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs". Molecular Pharmacology 43 (3): 320–7. PMID 7680751. 
  12. Ruat M, Traiffort E, Leurs R et al. (September 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. 
  13. Toll L, Berzetei-Gurske IP, Polgar WE et al. (March 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. 
  14. P K Gillman (July 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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