Isradipin
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Klinički podaci | |
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Prodajno ime | Clivoten, DynaCirc, Dynacirc CR, DynaCire |
Drugs.com | Monografija |
Način primene | Oralno |
Farmakokinetički podaci | |
Poluvreme eliminacije | 8 h |
Izlučivanje | Renalno (60-65%) |
Identifikatori | |
CAS broj | 75695-93-1 ![]() |
ATC kod | C08CA03 (WHO) |
PubChem | CID 3784 |
DrugBank | DB00270 ![]() |
ChemSpider | 3652 ![]() |
ChEMBL | CHEMBL1648 ![]() |
Hemijski podaci | |
Formula | C19H21N3O5 |
Molarna masa | 371,387 |
SMILES
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InChI
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Fizički podaci | |
Tačka topljenja | 168—170 °C (334—338 °F) |
Isradipin je organsko jedinjenje, koje sadrži 19 atoma ugljenika i ima molekulsku masu od 371,387 Da.[1][2][3][4][5][6]
Osobine
Osobina | Vrednost |
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Broj akceptora vodonika | 7 |
Broj donora vodonika | 1 |
Broj rotacionih veza | 6 |
Particioni koeficijent[7] (ALogP) | 2,2 |
Rastvorljivost[8] (logS, log(mol/L)) | -4,4 |
Polarna površina[9] (PSA, Å2) | 103,6 |
Stereokemija
Isradipin sadrži stereocentar i sastoji se od dva enantiomera, točnije atropizomera. Ovo je racemat, tj. Smjesa od 1: 1 ( R ) i ( S ) - oblika:[10]
Enantiomeri Isradipin | |
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![]() CAS-Nummer: 84260-63-9 | ![]() CAS-Nummer: 84260-64-0 |
Reference
- ^ Fletcher H, Roberts G, Mullings A, Forrester T: An open trial comparing isradipine with hydralazine and methyl dopa in the treatment of patients with severe pre-eclampsia. J Obstet Gynaecol. 1999 May;19(3):235-8. PMID 15512286
- ^ Ganz M, Mokabberi R, Sica DA: Comparison of blood pressure control with amlodipine and controlled-release isradipine: an open-label, drug substitution study. J Clin Hypertens (Greenwich). 2005 Apr;7 (4 Suppl 1):27-31. PMID 15858400
- ^ Hattori T, Wang PL: Calcium antagonist isradipine-induced calcium influx through nonselective cation channels in human gingival fibroblasts. Eur J Med Res. 2006 Mar 27;11(3):93-6. PMID 16751108
- ^ Johnson BA, Roache JD, Ait-Daoud N, Wallace C, Wells L, Dawes M, Wang Y: Effects of isradipine, a dihydropyridine-class calcium-channel antagonist, on d-methamphetamine's subjective and reinforcing effects. Int J Neuropsychopharmacol. 2005 Jun;8(2):203-13. PMID 15850499
- ^ 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. уреди
- ^ 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
. PMID 18048412. doi:10.1093/nar/gkm958. уреди
- ^ 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.
- ^ 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
- ^ 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
- ^ 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. 193.
Literatura
- Hardman JG, Limbird LE, Gilman AG (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10. изд.). New York: McGraw-Hill. ISBN 0071354697. doi:10.1036/0071422803.
- Thomas L. Lemke; David A. Williams, ур. (2007). Foye's Principles of Medicinal Chemistry (6. изд.). Baltimore: Lippincott Willams & Wilkins. ISBN 0781768799.
Spoljašnje veze
- Isradipine
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