WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H317884
CAS#: 52468-60-7
Description: Flunarizine is a non-selective calcium entry blocker with other actions including histamine H1 receptor blocking activity. It is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy. It may help to reduce the severity and duration of attacks of paralysis associated with the more serious form of alternating hemiplegia, as well as being effective in rapid onset dystonia-parkinsonism (both of these conditions share a mutation in the ATP13A gene). Flunarizine has also been shown to significantly reduce headache frequency and severity in both adults and children.
Hodoodo Cat#: H317884
Name: Flunarizine
CAS#: 52468-60-7
Chemical Formula: C15H14FN3O3
Exact Mass: 303.10
Molecular Weight: 303.288
Elemental Analysis: C, 59.40; H, 4.65; F, 6.26; N, 13.85; O, 15.83
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Synonym: Flunarizine, Sibelium, Flunarizina, Flunarizinum, Flunarizin, R-14950
IUPAC/Chemical Name: 1-[bis(4-fluorophenyl)methyl]-4-[(E)-3-phenylprop-2-enyl]piperazine
InChi Key: OFBIFZUFASYYRE-UHFFFAOYSA-N
InChi Code: InChI=1S/C15H14FN3O3/c1-3-22-15(21)13-12-7-18(2)14(20)10-6-9(16)4-5-11(10)19(12)8-17-13/h4-6,8H,3,7H2,1-2H3
SMILES Code: O=C(C1=C(CN2C)N(C=N1)C3=CC=C(F)C=C3C2=O)OCC
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | Flunarizine is a potent dual Na+/Ca2+ channel (T-type) blocker. |
| In vitro activity: | Application of FLN (flunarizine) produced a significant cytotoxic effect on U-87 MG (Fig. 1A), LN-229 (Fig. 1B), and U-118 MG (Fig. 1C) cells. The results of cell survival and colony formation assay suggested that FLN exhibited anti-proliferation activity in GBM cells. Reference: Eur J Pharmacol. 2021 Feb 5;892:173756. https://pubmed.ncbi.nlm.nih.gov/33245897/ |
| In vivo activity: | The flunarizine treatment significantly extended lifespan of ≈40% with a shift in mean survival of SMA mice (16.3 versus 11.7 days; Mantel-Cox test, p = 0.0002). Reference: Sci Rep. 2018; 8: 2075. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5794986/ |
The following data is based on the product molecular weight 303.29 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Kim HJ, Lee J, Lee GR, Kim N, Lee HI, Kwon M, Kim NY, Park JH, Kang YH, Song HJ, Kim T, Shin DM, Jeong W. Flunarizine inhibits osteoclastogenesis by regulating calcium signaling and promotes osteogenesis. J Cell Physiol. 2021 Jun 30. doi: 10.1002/jcp.30496. Epub ahead of print. PMID: 34192358. 2. Chen SH, Chao CN, Chen SY, Lin HP, Huang HY, Fang CY. Flunarizine, a drug approved for treating migraine and vertigo, exhibits cytotoxicity in GBM cells. Eur J Pharmacol. 2021 Feb 5;892:173756. doi: 10.1016/j.ejphar.2020.173756. Epub 2020 Nov 25. PMID: 33245897. 3. Sapaly D, Dos Santos M, Delers P, Biondi O, Quérol G, Houdebine L, Khoobarry K, Girardet F, Burlet P, Armand AS, Chanoine C, Bureau JF, Charbonnier F, Lefebvre S. Small-molecule flunarizine increases SMN protein in nuclear Cajal bodies and motor function in a mouse model of spinal muscular atrophy. Sci Rep. 2018 Feb 1;8(1):2075. doi: 10.1038/s41598-018-20219-1. PMID: 29391529; PMCID: PMC5794986. |
| In vitro protocol: | 1. Kim HJ, Lee J, Lee GR, Kim N, Lee HI, Kwon M, Kim NY, Park JH, Kang YH, Song HJ, Kim T, Shin DM, Jeong W. Flunarizine inhibits osteoclastogenesis by regulating calcium signaling and promotes osteogenesis. J Cell Physiol. 2021 Jun 30. doi: 10.1002/jcp.30496. Epub ahead of print. PMID: 34192358. 2. Chen SH, Chao CN, Chen SY, Lin HP, Huang HY, Fang CY. Flunarizine, a drug approved for treating migraine and vertigo, exhibits cytotoxicity in GBM cells. Eur J Pharmacol. 2021 Feb 5;892:173756. doi: 10.1016/j.ejphar.2020.173756. Epub 2020 Nov 25. PMID: 33245897. |
| In vivo protocol: | 1. Kim HJ, Lee J, Lee GR, Kim N, Lee HI, Kwon M, Kim NY, Park JH, Kang YH, Song HJ, Kim T, Shin DM, Jeong W. Flunarizine inhibits osteoclastogenesis by regulating calcium signaling and promotes osteogenesis. J Cell Physiol. 2021 Jun 30. doi: 10.1002/jcp.30496. Epub ahead of print. PMID: 34192358. 2. Sapaly D, Dos Santos M, Delers P, Biondi O, Quérol G, Houdebine L, Khoobarry K, Girardet F, Burlet P, Armand AS, Chanoine C, Bureau JF, Charbonnier F, Lefebvre S. Small-molecule flunarizine increases SMN protein in nuclear Cajal bodies and motor function in a mouse model of spinal muscular atrophy. Sci Rep. 2018 Feb 1;8(1):2075. doi: 10.1038/s41598-018-20219-1. PMID: 29391529; PMCID: PMC5794986. |
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8: McLean MJ. In vitro electrophysiological evidence predicting anticonvulsant efficacy of memantine and flunarizine. Pol J Pharmacol Pharm. 1987 Sep-Oct;39(5):513-25. Review. PubMed PMID: 3333611.
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10: Wouters L, Amery W, Towse G. Flunarizine in the treatment of vertigo. J Laryngol Otol. 1983 Aug;97(8):697-704. Review. PubMed PMID: 6350513.
11: Amery WK. Flunarizine, a calcium channel blocker: a new prophylactic drug in migraine. Headache. 1983 Mar;23(2):70-4. Review. PubMed PMID: 6343298.
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16: Lastra Martínez L, Herranz Fernández J, Arteaga Manjón-Cabez R. [Flunarizine and dihydroergotamine in the treatment of migraine in children]. An Esp Pediatr. 1990 Mar;32(3):213-8. Review. Spanish. Erratum in: An Esp Pediatr 1990 Jun;32(6):566. PubMed PMID: 2189328.
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18: Bakchine S, Lacomblez L, Soubrié C. [Extrapyramidal syndrome during treatment with flunarizine]. Rev Neurol (Paris). 1988;144(12):833-4. Review. French. PubMed PMID: 3070697.
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