Etosuksimid

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Etosuksimid
Klinički podaci
Robne marke Asamid, Atysmal, Capitus, Emeside
AHFS/Drugs.com Monografija
Identifikatori
CAS broj 77-67-8
ATC kod N03AD01
PubChem[1][2] 3291
DrugBank DB00593
ChemSpider[3] 3175
KEGG[4] C07505 YesY
ChEBI CHEBI:4887 YesY
ChEMBL[5] CHEMBL696 YesY
Hemijski podaci
Formula C7H11NO2 
Mol. masa 141,168
SMILES eMolekuli & PubHem
Fizički podaci
Tačka topljenja 64.5 °C (148 °F)
Farmakokinetički podaci
Poluvreme eliminacije 53 h
Farmakoinformacioni podaci
Trudnoća ?
Pravni status
Način primene Oralno

Etosuksimid je organsko jedinjenje, koje sadrži 7 atoma ugljenika i ima molekulsku masu od 141,168 Da.[6][7][8][9][10][11][12]

Osobine[uredi - уреди | uredi izvor]

Osobina Vrednost
Broj akceptora vodonika 2
Broj donora vodonika 1
Broj rotacionih veza 1
Particioni koeficijent[13] (ALogP) 0,5
Rastvorljivost[14] (logS, log(mol/L)) -1,1
Polarna površina[15] (PSA, Å2) 46,2

Stereokemija[uredi - уреди | uredi izvor]

Ethosuximid je kiralni lijek s stereocenterom. Terapeutski se koristi racemat, 1: 1 smjesa ( S ) i ( R ) izomera.[16]

Enantiomeri etosuksimida
(R)-Ethosuximid Structural Formula V1.svg
CAS-Nummer: 39122-20-8
(S)-Ethosuximid Structural Formula V1.svg
CAS-Nummer: 39122-19-5

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. Patsalos PN: Properties of antiepileptic drugs in the treatment of idiopathic generalized epilepsies. Epilepsia. 2005;46 Suppl 9:140-8. PMID 16302888
  7. Coulter DA, Huguenard JR, Prince DA: Specific petit mal anticonvulsants reduce calcium currents in thalamic neurons. Neurosci Lett. 1989 Mar 13;98(1):74-8. PMID 2710401
  8. Coulter DA, Huguenard JR, Prince DA: Characterization of ethosuximide reduction of low-threshold calcium current in thalamic neurons. Ann Neurol. 1989 Jun;25(6):582-93. PMID 2545161
  9. Coulter DA, Huguenard JR, Prince DA: Differential effects of petit mal anticonvulsants and convulsants on thalamic neurones: calcium current reduction. Br J Pharmacol. 1990 Aug;100(4):800-6. PMID 2169941
  10. Kostyuk PG, Molokanova EA, Pronchuk NF, Savchenko AN, Verkhratsky AN: Different action of ethosuximide on low- and high-threshold calcium currents in rat sensory neurons. Neuroscience. 1992 Dec;51(4):755-8. PMID 1336826
  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 3013709. PMID 21059682. doi:10.1093/nar/gkq1126. 
  12. David S. Wishart, Craig Knox, An Chi Guo, Dean Cheng, Savita Shrivastava, Dan Tzur, Bijaya Gautam, and Murtaza Hassanali (2008). "DrugBank: a knowledgebase for drugs, drug actions and drug targets". Nucleic acids research 36 (Database issue): D901–6. PMC 2238889. PMID 18048412. doi:10.1093/nar/gkm958. 
  13. Ghose, A.K., Viswanadhan V.N., and 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. 
  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. 
  16. Rote Liste Service GmbH (Hrsg.): Rote Liste 2017 – Arzneimittelverzeichnis für Deutschland (einschließlich EU-Zulassungen und bestimmter Medizinprodukte). Rote Liste Service GmbH, Frankfurt/Main, 2017, Aufl. 57, ISBN 978-3-946057-10-9, S. 182.

Literatura[uredi - уреди | uredi izvor]

Spoljašnje veze[uredi - уреди | uredi izvor]

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