Felodipine

  • CAT Number: A001024
  • CAS Number: 72509-76-3
  • Molecular Formula: C18H19Cl2NO4
  • Molecular Weight: 384.3
  • Purity: ≥95%
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Felodipine (CAS 72509-76-3) is a calcium channel blocker (calcium antagonist), used to control hypertension. Felodipine prevents calcium from being released within the muscle cells of the small arteries and thereby causes the muscles to relax and the arteries to dilate or expand. Dilation of arteries reduces blood pressure. Felodipine has little or no effect on the muscles of veins or the heart. Felodipine was approved by the FDA in 1991.

Catalog Number A001024
CAS Number 72509-76-3
Synonyms

72509-76-3; Plendil; Flodil; Munobal; Renedil

Molecular Formula

C18H19Cl2NO4

Purity 95%
Target Calcium Channel
Solubility >17.7mg/mL in DMSO
Storage -20°C
IUPAC Name 5-O-ethyl 3-O-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate
InChI 1S/C18H19Cl2NO4/c1-5-25-18(23)14-10(3)21-9(2)13(17(22)24-4)15(14)11-7-6-8-12(19)16(11)20/h6-8,15,21H,5H2,1-4H3
InChIKey RZTAMFZIAATZDJ-UHFFFAOYSA-N
SMILES CCOC(=O)C1=C(NC(=C(C1C2=C(C(=CC=C2)Cl)Cl)C(=O)OC)C)C
Reference

1: Palazi E, Karavas E, Barmpalexis P, Kostoglou M, Nanaki S, Christodoulou E, Bikiaris DN. Melt extrusion process for adjusting drug release of poorly water soluble drug felodipine using different polymer matrices. Eur J Pharm Sci. 2018 Jan 3;114:332-345. doi: 10.1016/j.ejps.2018.01.004. [Epub ahead of print] PubMed PMID: 29305982.<br />
2: Fu J, Cui L, Yang C, Xiong H, Ren G, Ma X, Jing Q, Ren F. Screen for Inhibitors of Crystal Growth to Identify Desirable Carriers for Amorphous Solid Dispersions Containing Felodipine. AAPS PharmSciTech. 2018 Jan 4. doi: 10.1208/s12249-017-0942-7. [Epub ahead of print] PubMed PMID: 29302871.<br />
3: Singh M, Kanoujia J, Parashar P, Arya M, Tripathi CB, Sinha VR, Saraf SK, Saraf SA. Augmented bioavailability of felodipine through an &alpha;-linolenic acid-based microemulsion. Drug Deliv Transl Res. 2018 Feb;8(1):204-225. doi: 10.1007/s13346-017-0453-9. PubMed PMID: 29204927.<br />
4: Ren F, Fu J, Xiong H, Cui L, Ren G, Guan H, Jing Q. Complexes of Felodipine Nanoparticles With Zein Prepared Using a Dual Shift Technique. J Pharm Sci. 2018 Jan;107(1):239-249. doi: 10.1016/j.xphs.2017.09.031. Epub 2017 Oct 28. PubMed PMID: 29107791.<br />
5: Li D, Xu S, Wang Y, Li D, Li X, Pan J, Xu P. Pharmacokinetics and drug-drug interaction between enalapril, enalaprilat and felodipine extended release (ER) in healthy subjects. Oncotarget. 2017 Aug 7;8(41):70752-70760. doi: 10.18632/oncotarget.19984. eCollection 2017 Sep 19. PubMed PMID: 29050316; PubMed Central PMCID: PMC5642591.<br />
6: Qi J, Zheng JB, Ai WT, Yao XW, Liang L, Cheng G, Shou XL, Sun CF. Felodipine inhibits ox-LDL-induced reactive oxygen species production and inflammation in human umbilical vein endothelial cells. Mol Med Rep. 2017 Oct;16(4):4871-4878. doi: 10.3892/mmr.2017.7181. Epub 2017 Aug 7. PubMed PMID: 28791379.<br />
7: Chen M, Zhou J, Mei L, Yu F, Xie X, Liu Y, Yang Y, Li Y, Mei X. Simultaneous Determination of Felodipine and Metoprolol in Beagle Dog Plasma by Online SPE-LC-MS/MS and Its Application in a Pharmacokinetic Study. Anal Sci. 2017;33(7):755-759. doi: 10.2116/analsci.33.755. PubMed PMID: 28690250.<br />
8: Tanaka KI, Niino T, Ishihara T, Takafuji A, Takayama T, Kanda Y, Sugizaki T, Tamura F, Kurotsu S, Kawahara M, Mizushima T. Protective and therapeutic effect of felodipine against bleomycin-induced pulmonary fibrosis in mice. Sci Rep. 2017 Jun 13;7(1):3439. doi: 10.1038/s41598-017-03676-y. PubMed PMID: 28611390; PubMed Central PMCID: PMC5469778.<br />
9: Sayed S, Habib BA, Elsayed GM. Tri-block co-polymer nanocarriers for enhancement of oral delivery of felodipine: preparation, in vitro characterization and ex vivo permeation. J Liposome Res. 2017 May 25:1-11. doi: 10.1080/08982104.2017.1327541. [Epub ahead of print] PubMed PMID: 28480807.<br />
10: Geroge JK, Verma PRP, Venkatesan J, Lee JY, Yoon DH, Kim SK, Singh SK. Studies on Core-Shell Nanocapsules of Felodipine: In Vitro-In Vivo Evaluations. AAPS PharmSciTech. 2017 Nov;18(8):2871-2888. doi: 10.1208/s12249-017-0770-9. Epub 2017 Apr 19. PubMed PMID: 28424979.

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