Etosuksimid

Etosuksimid
Klinički podaci
Prodajno imeAsamid, Atysmal, Capitus, Emeside
Drugs.comMonografija
Način primeneOralno
Farmakokinetički podaci
Poluvreme eliminacije53 h
Identifikatori
CAS broj77-67-8 ДаY
ATC kodN03AD01 (WHO)
PubChemCID 3291
DrugBankDB00593 ДаY
ChemSpider3175 ДаY
KEGGC07505 ДаY
ChEBICHEBI:4887 ДаY
ChEMBLCHEMBL696 ДаY
Hemijski podaci
FormulaC7H11NO2
Molarna masa141,168
  • CCC1(C)CC(=O)NC1=O
  • InChI=1S/C7H11NO2/c1-3-7(2)4-5(9)8-6(7)10/h3-4H2,1-2H3,(H,8,9,10) ДаY
  • Key:HAPOVYFOVVWLRS-UHFFFAOYSA-N ДаY
Fizički podaci
Tačka topljenja645 °C (1.193 °F)

Etosuksimid je organsko jedinjenje, koje sadrži 7 atoma ugljenika i ima molekulsku masu od 141,168 Da.[1][2][3][4][5][6][7]

Osobine

Osobina Vrednost
Broj akceptora vodonika 2
Broj donora vodonika 1
Broj rotacionih veza 1
Particioni koeficijent[8] (ALogP) 0,5
Rastvorljivost[9] (logS, log(mol/L)) -1,1
Polarna površina[10] (PSA, Å2) 46,2

Stereohemija

Ethosuksimid je hiralni lek s stereocenterom. Terapeutski se koristi racemat, 1: 1 smeša ( S ) i ( R ) izomera.[11]

Enantiomeri etosuksimida

CAS-Nummer: 39122-20-8
CAS-Nummer: 39122-19-5

Reference

  1. ^ Patsalos PN: Properties of antiepileptic drugs in the treatment of idiopathic generalized epilepsies. Epilepsia. 2005;46 Suppl 9:140-8. PMID 16302888
  2. ^ 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
  3. ^ 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
  4. ^ 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
  5. ^ 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
  6. ^ 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 Слободан приступ. PMID 21059682. doi:10.1093/nar/gkq1126. 
  7. ^ 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 2238889 Слободан приступ. PMID 18048412. doi:10.1093/nar/gkm958. 
  8. ^ 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. 
  9. ^ 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. 
  10. ^ 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. 
  11. ^ 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

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