Fipamezole  (Synonyms: MPV 1730; JP-1730)

Fipamezole (MPV 1730; JP-1730) is a potent and orally active α2-adrenergic receptor antagonist with K_i 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 functional assays, the potent antagonist properties of Fipamezole (JP-1730) are demonstrated by its ability to reduce adrenaline-induced ³⁵S-GTPγS binding with K_B values of 8.4 nM, 16 nM, 4.7 nM at human α2A, α2B, and α2C receptors, respectively. Fipamezole also has moderate affinity at histamine H1 and H3 receptors and the serotonin (5-HT) transporter (IC₅₀ of 100 nM-1 μM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

230.28

C₁₄H₁₅FN₂

150586-58-6

FC1=CC=C2C(CC(C2)(CC)C3=CN=CN3)=C1

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• [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.  [Content Brief]