| Identification | Back Directory | [Name]
4-(2-ethyl-5-fluoro-1,3-dihydroinden-2-yl)-3H-imidazole | [CAS]
150586-58-6 | [Synonyms]
JP1730
JP-1730
JP 1730
fipamezole
4-(2-ethyl-5-fluoro-1,3-dihydroinden-2-yl)-3H-imidazole
1H-Imidazole, 5-(2-ethyl-5-fluoro-2,3-dihydro-1H-inden-2-yl)- | [Molecular Formula]
C14H15FN2 | [MDL Number]
MFCD00922400 | [MOL File]
150586-58-6.mol | [Molecular Weight]
230.28 |
| Hazard Information | Back Directory | [Uses]
Fipamezole (MPV 1730; JP-1730) is a potent and orally active α2-adrenergic receptor antagonist with Ki values of 9.2 nM, 17 nM, and 55 nM for human α2A, α2B, and α2C, receptors, respectively. Fipamezole is an anti-dyskinetic agent, and can be used for the study of Parkinson's disease[1]. | [in vivo]
In the MPTP-lesioned marmoset, Fipamezole (1-10 mg/kg; po; once) significantly reduces L-dopa-induced dyskinesia without compromising the anti-parkinsonian action of L-DOPA (HY-N0304)[1]. | Animal Model: | Adult common marmosets (Callithrix jacchus, 300-345 g) injected with MPTP hydrochloride (2 mg/kg) and L-DOPA (8 mg/kg)[1] | | Dosage: | 1 mg/kg, 3 mg/kg, 10 mg/kg | | Administration: | po; once | | Result: | Significantly reduced L-DOPA-induced dyskinesia. |
| [IC 50]
human α2A-adrenoceptor: 9.2 nM (Ki); human α2B-adrenoceptor: 17 nM (Ki); human α2C-adrenoceptor: 55 nM (Ki) | [References]
[1] Juha-Matti Savola, et al. 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. DOI:10.1002/mds.10464 |
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