WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H528807
CAS#: 150586-72-4 (Fipamezole HCl)
Description: Fipamezole HCl is a α2-adrenoceptor antagonist potentially for the treatment of dyskinesia associated with Parkinson's disease.
Hodoodo Cat#: H528807
Name: Fipamezole HCl
CAS#: 150586-72-4 (Fipamezole HCl)
Chemical Formula: C14H16ClFN2
Exact Mass: 0.00
Molecular Weight: 266.740
Elemental Analysis: C, 63.04; H, 6.05; Cl, 13.29; F, 7.12; N, 10.50
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Related CAS #: 150586-58-6 (Fipamezole free base)
Synonym: MPV-1730; JP-1730; MPV1730; JP1730; MPV 1730; JP 1730
IUPAC/Chemical Name: 4-(2-ethyl-5-fluoro-2,3-dihydro-1H-inden-2-yl)-1H-imidazole hydrochloride
InChi Key: XAGTWPPXXHAZMK-UHFFFAOYSA-N
InChi Code: InChI=1S/C14H15FN2.ClH/c1-2-14(13-8-16-9-17-13)6-10-3-4-12(15)5-11(10)7-14;/h3-5,8-9H,2,6-7H2,1H3,(H,16,17);1H
SMILES Code: FC1=CC2=C(CC(C3=CNC=N3)(CC)C2)C=C1.[H]Cl
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
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: | |
In vitro activity: | |
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The following data is based on the product molecular weight 266.74 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: | |
In vitro protocol: | |
In vivo protocol: |
1: Lewitt PA, Hauser RA, Lu M, Nicholas AP, Weiner W, Coppard N, Leinonen M, Savola JM. Randomized clinical trial of fipamezole for dyskinesia in Parkinson disease (FJORD study). Neurology. 2012 Jul 10;79(2):163-9. doi: 10.1212/WNL.0b013e31825f0451. PubMed PMID: 22744665.
2: Johnston TH, Fox SH, Piggott MJ, Savola JM, Brotchie JM. The α₂ adrenergic antagonist fipamezole improves quality of levodopa action in Parkinsonian primates. Mov Disord. 2010 Oct 15;25(13):2084-93. doi: 10.1002/mds.23172. PubMed PMID: 20824735.
3: Savola JM, Hill M, Engstrom M, Merivuori H, Wurster S, McGuire SG, Fox SH, Crossman AR, Brotchie JM. Fipamezole (JP-1730) is a potent alpha2 adrenergic receptor antagonist that reduces levodopa-induced dyskinesia in the MPTP-lesioned primate model of Parkinson's disease. Mov Disord. 2003 Aug;18(8):872-83. PubMed PMID: 12889076.
4: Pilleri M, Antonini A. Therapeutic strategies to prevent and manage dyskinesias in Parkinson's disease. Expert Opin Drug Saf. 2015 Feb;14(2):281-94. doi: 10.1517/14740338.2015.988137. Review. PubMed PMID: 25483147.
5: Fox SH. Non-dopaminergic treatments for motor control in Parkinson's disease. Drugs. 2013 Sep;73(13):1405-15. doi: 10.1007/s40265-013-0105-4. Review. Erratum in: Drugs. 2014 Jul;74(11):1305. PubMed PMID: 23917951.
6: Pytka K, Zygmunt M, Filipek B. [Pharmacotherapy of Parkinson's disease: progress or regress?]. Postepy Hig Med Dosw (Online). 2013 Jul 24;67:700-8. Review. Polish. PubMed PMID: 24018435.
7: Perez-Lloret S, Rey MV, Pavy-Le Traon A, Rascol O. Emerging drugs for autonomic dysfunction in Parkinson's disease. Expert Opin Emerg Drugs. 2013 Mar;18(1):39-53. doi: 10.1517/14728214.2013.766168. Review. PubMed PMID: 23373820.
8: Hauser RA. Future treatments for Parkinson's disease: surfing the PD pipeline. Int J Neurosci. 2011;121 Suppl 2:53-62. doi: 10.3109/00207454.2011.620195. Review. PubMed PMID: 22035030.
9: Bayes M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Jun;25(5):387-408. PubMed PMID: 12851663.
10: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2006 Oct;28(8):533-91. PubMed PMID: 17136234.
11: Fox SH, Lang AE, Brotchie JM. Translation of nondopaminergic treatments for levodopa-induced dyskinesia from MPTP-lesioned nonhuman primates to phase IIa clinical studies: keys to success and roads to failure. Mov Disord. 2006 Oct;21(10):1578-94. Review. PubMed PMID: 16874752.
12: Johnston TH, Brotchie JM. Drugs in development for Parkinson's disease. Curr Opin Investig Drugs. 2004 Jul;5(7):720-6. Review. PubMed PMID: 15298067.
13: Santhera licenses novel dyskinesia therapy to Biovail. Nat Rev Drug Discov. 2009 Oct;8(10):762. doi: 10.1038/nrd3009. PubMed PMID: 19794436.