Klevidipin

Klevidipin
Klinički podaci
AHFS/Drugs.com Monografija
Identifikatori
CAS broj 166432-28-6
ATC kod nije dodeljen
PubChem[1][2] 193993
DrugBank DB04920
ChemSpider[3] 168334
ChEMBL[4] CHEMBL1201762 DaY
Hemijski podaci
Formula C21H23Cl2NO6 
Mol. masa 456,316
SMILES eMolekuli & PubHem
Farmakokinetički podaci
Poluvreme eliminacije 1 minut
Izlučivanje urin 63-74%,
Farmakoinformacioni podaci
Trudnoća ?
Pravni status
Način primene Intravenozno

Klevidipin je organsko jedinjenje, koje sadrži 21 atom ugljenika i ima molekulsku masu od 456,316 Da.[5][6][7][8][9][10]

Osobine

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Osobina Vrednost
Broj akceptora vodonika 7
Broj donora vodonika 1
Broj rotacionih veza 10
Particioni koeficijent[11] (ALogP) 4,1
Rastvorljivost[12] (logS, log(mol/L)) -6,1
Polarna površina[13] (PSA, Å2) 90,9

Stereokemija

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Klevidipin sadrži stereocentar i sastoji se od dva enantiomera. Ovo je racemat, tj. 1: 1 smjesa ( R ) i ( S ) - oblika:[14]

Enantiomeri Klevidipin

CAS-Nummer: 167356-40-3

CAS-Nummer: 167356-39-0

Reference

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  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. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  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. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. 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. DOI:10.1093/nar/gkr777. PMID 21948594.  edit
  5. Zhang JG, Dehal SS, Ho T, Johnson J, Chandler C, Blanchard AP, Clark RJ Jr, Crespi CL, Stresser DM, Wong J: Human cytochrome p450 induction and inhibition potential of clevidipine and its primary metabolite h152/81. Drug Metab Dispos. 2006 May;34(5):734-7. Epub 2006 Feb 24. PMID 16501008
  6. Nordlander M, Sjoquist PO, Ericsson H, Ryden L: Pharmacodynamic, pharmacokinetic and clinical effects of clevidipine, an ultrashort-acting calcium antagonist for rapid blood pressure control. Cardiovasc Drug Rev. 2004 Fall;22(3):227-50. PMID 15492770
  7. Wang QD, Segawa D, Ericsson H, Sjoquist PO, Johansson L, Ryden L: Time-dependent cardioprotection with calcium antagonism and experimental studies with clevidipine in ischemic-reperfused pig hearts: part I. J Cardiovasc Pharmacol. 2002 Aug;40(2):228-34. PMID 12131552
  8. Stephens CT, Jandhyala BS: Effects of fenoldopam, a dopamine D-1 agonist, and clevidipine, a calcium channel antagonist, in acute renal failure in anesthetized rats. Clin Exp Hypertens. 2002 May;24(4):301-13. PMID 12069360
  9. 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. DOI:10.1093/nar/gkq1126. PMC 3013709. PMID 21059682.  edit
  10. 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 Res 36 (Database issue): D901-6. DOI:10.1093/nar/gkm958. PMC 2238889. PMID 18048412.  edit
  11. 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. 
  12. 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. DOI:10.1021/ci000392t. PMID 11749573.  edit
  13. 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. DOI:10.1021/jm000942e. PMID 11020286.  edit
  14. 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. 171.

Literatura

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Spoljašnje veze

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