Isradipin
-Isradipin_Structural_Formula_V1.svg)
| |||
| Klinički podaci | |||
|---|---|---|---|
| Robne marke | Clivoten, DynaCirc, Dynacirc CR, DynaCire | ||
| AHFS/Drugs.com | Monografija | ||
| Identifikatori | |||
| CAS broj | 75695-93-1 | ||
| ATC kod | C08CA03 | ||
| PubChem[1][2] | 3784 | ||
| DrugBank | DB00270 | ||
| ChemSpider[3] | 3652 | ||
| ChEMBL[4] | CHEMBL1648 
| ||
| Hemijski podaci | |||
| Formula | C19H21N3O5 | ||
| Mol. masa | 371,387 | ||
| SMILES | eMolekuli & PubHem | ||
| |||
| Fizički podaci | |||
| Tačka topljenja | 168-170 °C (-106 °F) | ||
| Farmakokinetički podaci | |||
| Poluvreme eliminacije | 8 h | ||
| Izlučivanje | Renalno (60-65%) | ||
| Farmakoinformacioni podaci | |||
| Trudnoća | ? | ||
| Pravni status | |||
| Način primene | Oralno | ||
Isradipin je organsko jedinjenje, koje sadrži 19 atoma ugljenika i ima molekulsku masu od 371,387 Da.[5][6][7][8][9][10]
| Osobina | Vrednost |
|---|---|
| Broj akceptora vodonika | 7 |
| Broj donora vodonika | 1 |
| Broj rotacionih veza | 6 |
| Particioni koeficijent[11] (ALogP) | 2,2 |
| Rastvorljivost[12] (logS, log(mol/L)) | -4,4 |
| Polarna površina[13] (PSA, Å2) | 103,6 |
Isradipin sadrži stereocentar i sastoji se od dva enantiomera, točnije atropizomera. Ovo je racemat, tj. Smjesa od 1: 1 ( R ) i ( S ) - oblika:[14]
| Enantiomeri Isradipin | |
|---|---|
-Isradipin_Structural_Formula_V1.svg) CAS-Nummer: 84260-63-9 |
-Isradipin_Structural_Formula_V1.svg) CAS-Nummer: 84260-64-0 |
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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. DOI:10.1093/nar/gkq1126. PMC 3013709. PMID 21059682.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- Hardman JG, Limbird LE, Gilman AG. (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10 izd.). New York: McGraw-Hill. DOI:10.1036/0071422803. ISBN 0-07-135469-7.
- Thomas L. Lemke, David A. Williams, ur. (2007). Foye's Principles of Medicinal Chemistry (6 izd.). Baltimore: Lippincott Willams & Wilkins. ISBN 0-7817-6879-9.
