Klevidipin

Klevidipin
Klinički podaci
Drugs.comMonografija
Način primeneIntravenozno
Farmakokinetički podaci
Poluvreme eliminacije1 minut
Izlučivanjeurin 63-74%,
Identifikatori
CAS broj166432-28-6 ДаY
ATC kodNone
PubChemCID 193993
DrugBankDB04920 ДаY
ChemSpider168334 ДаY
ChEMBLCHEMBL1201762 ДаY
Hemijski podaci
FormulaC21H23Cl2NO6
Molarna masa456,316
  • CCCC(=O)OCOC(=O)C1=C(C)NC(C)=C(C1C1=CC=CC(Cl)=C1Cl)C(=O)OC
  • InChI=1S/C21H23Cl2NO6/c1-5-7-15(25)29-10-30-21(27)17-12(3)24-11(2)16(20(26)28-4)18(17)13-8-6-9-14(22)19(13)23/h6,8-9,18,24H,5,7,10H2,1-4H3 ДаY
  • Key:KPBZROQVTHLCDU-UHFFFAOYSA-N ДаY

Klevidipin je organsko jedinjenje, koje sadrži 21 atom ugljenika i ima molekulsku masu od 456,316 Da.[1][2][3][4][5][6]

Osobine

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Osobina Vrednost
Broj akceptora vodonika 7
Broj donora vodonika 1
Broj rotacionih veza 10
Particioni koeficijent[7] (ALogP) 4,1
Rastvorljivost[8] (logS, log(mol/L)) -6,1
Polarna površina[9] (PSA, Å2) 90,9

Stereohemija

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Klevidipin sadrži stereocentar i sastoji se od dva enantiomera. Ovo je racemat, tj. 1: 1 smeša ( R ) i ( S ) - oblika:[10]

Enantiomeri Klevidipina

CAS-Nummer: 167356-40-3
CAS-Nummer: 167356-39-0

Reference

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  1. ^ 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
  2. ^ 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
  3. ^ 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
  4. ^ 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
  5. ^ 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.  уреди
  6. ^ 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.  уреди
  7. ^ 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. 
  8. ^ 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
  9. ^ 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
  10. ^ 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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Klevidipin на Викимедијиној остави.