Retigabin

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Retigabin
Retigabine.svg
Retigabine3D1.png
Klinički podaci
Drugs.comMonografija
Način primeneOralno
Farmakokinetički podaci
Poluvreme eliminacije7,5 h
IzlučivanjeRenalno (85%)
Identifikatori
CAS broj150812-12-7 ДаY
ATC kodN03AX21 (WHO)
PubChemCID 121892
DrugBankDB04953 ДаY
ChemSpider108740 ДаY
KEGGC13826 ДаY
ChEBICHEBI:68584 ДаY
ChEMBLCHEMBL41355 ДаY
Hemijski podaci
FormulaC16H18FN3O2
Molarna masa303,331

Retigabin je organsko jedinjenje, koje sadrži 16 atoma ugljenika i ima molekulsku masu od 303,331 Da.[1][2][3][4][5][6][7][8][9][10][11][12]

Osobine[уреди]

Osobina Vrednost
Broj akceptora vodonika 4
Broj donora vodonika 3
Broj rotacionih veza 6
Particioni koeficijent[13] (ALogP) 2,8
Rastvorljivost[14] (logS, log(mol/L)) -4,3
Polarna površina[15] (PSA, Å2) 76,4

Reference[уреди]

  1. ^ Porter RJ, Nohria V, Rundfeldt C: Retigabine. Neurotherapeutics. 2007 Jan;4(1):149-54. PMID 17199031
  2. ^ Hermann R, Ferron GM, Erb K, Knebel N, Ruus P, Paul J, Richards L, Cnota HP, Troy S: Effects of age and sex on the disposition of retigabine. Clin Pharmacol Ther. 2003 Jan;73(1):61-70. PMID 12545144
  3. ^ Hermann R, Knebel NG, Niebch G, Richards L, Borlak J, Locher M: Pharmacokinetic interaction between retigabine and lamotrigine in healthy subjects. Eur J Clin Pharmacol. 2003 Apr;58(12):795-802. Epub 2003 Feb 28. PMID 12698305
  4. ^ Dost R, Rostock A, Rundfeldt C: The anti-hyperalgesic activity of retigabine is mediated by KCNQ potassium channel activation. Naunyn Schmiedebergs Arch Pharmacol. 2004 Apr;369(4):382-90. Epub 2004 Mar 9. PMID 15007538
  5. ^ Mikkelsen JD: The KCNQ channel activator retigabine blocks haloperidol-induced c-Fos expression in the striatum of the rat. Neurosci Lett. 2004 May 27;362(3):240-3. PMID 15158023
  6. ^ Punke MA, Friederich P: Retigabine stimulates human KCNQ2/Q3 channels in the presence of bupivacaine. Anesthesiology. 2004 Aug;101(2):430-8. PMID 15277926
  7. ^ Wuttke TV, Seebohm G, Bail S, Maljevic S, Lerche H: The new anticonvulsant retigabine favors voltage-dependent opening of the Kv7.2 (KCNQ2) channel by binding to its activation gate. Mol Pharmacol. 2005 Apr;67(4):1009-17. Epub 2005 Jan 20. PMID 15662042
  8. ^ Fatope MO: Retigabine (ASTA Medica). IDrugs. 2001 Jan;4(1):93-8. PMID 16034707
  9. ^ Orhan G, Wuttke TV, Nies AT, Schwab M, Lerche H: Retigabine/Ezogabine, a KCNQ/K(V)7 channel opener: pharmacological and clinical data. Expert Opin Pharmacother. 2012 Aug;13(12):1807-16. doi: 10.1517/14656566.2012.706278. Epub 2012 Jul 12. PMID 22783830
  10. ^ Amabile CM, Vasudevan A: Ezogabine: a novel antiepileptic for adjunctive treatment of partial-onset seizures. Pharmacotherapy. 2013 Feb;33(2):187-94. doi: 10.1002/phar.1185. PMID 23386597
  11. ^ Knox C, Law V, Jewison T, Liu P, Ly S, Frolkis A, Pon A, Banco K, Mak C, Neveu V, Djoumbou Y, Eisner R, Guo AC, Wishart DS (2011). „DrugBank 3.0: a comprehensive resource for omics research on drugs”. Nucleic Acids Res. 39 (Database issue): D1035—41. PMC 3013709Слободан приступ. PMID 21059682. doi:10.1093/nar/gkq1126.  уреди
  12. ^ David S. Wishart; Craig Knox; An Chi Guo; Dean Cheng; Savita Shrivastava; Dan Tzur; Bijaya Gautam; Murtaza Hassanali (2008). „DrugBank: a knowledgebase for drugs, drug actions and drug targets”. Nucleic acids research. 36 (Database issue): D901—6. PMC 2238889Слободан приступ. PMID 18048412. doi:10.1093/nar/gkm958.  уреди
  13. ^ Ghose, A.K.; Viswanadhan V.N. & Wendoloski, J.J. (1998). „Prediction of Hydrophobic (Lipophilic) Properties of Small Organic Molecules Using Fragment Methods: An Analysis of AlogP and CLogP Methods”. J. Phys. Chem. A. 102: 3762—3772. doi:10.1021/jp980230o. 
  14. ^ Tetko IV, Tanchuk VY, Kasheva TN, Villa AE (2001). „Estimation of Aqueous Solubility of Chemical Compounds Using E-State Indices”. Chem Inf. Comput. Sci. 41: 1488—1493. PMID 11749573. doi:10.1021/ci000392t.  уреди
  15. ^ Ertl P.; Rohde B.; Selzer P. (2000). „Fast calculation of molecular polar surface area as a sum of fragment based contributions and its application to the prediction of drug transport properties”. J. Med. Chem. 43: 3714—3717. PMID 11020286. doi:10.1021/jm000942e.  уреди

Literatura[уреди]

Spoljašnje veze[уреди]

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