Fipamezole

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 Vitro: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]. 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].