Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist (Ki=2.2 nM) in experimental models of Parkinson's disease.
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A2A receptor (A2AR) with Ki of 2.2 nM. The affinity of it for the A2AR is 70-fold greater than that for the A1 receptor [11]. Istradefylline binds to A1R, A2AR, and A3R in human with Kis of >287 nM, 9.12 nM, and >681 nM, respectively, 50.9 nM and 1.57 nM for A1R and A2AR in rat, 105.02 nM and 1.87 nM for A1R and A2AR in mouse, respectively [6]. Istradefylline causes concentration-dependent abolition of bFGF induction of astrogliosis in primary rat striatal astrocytes [7]. The ED50s of istradefylline in the reversal of CGS21680-induced and reserpine-induced catalepsy were 0.05 mg/kg, PO and 0.26 mg/kg, PO, respectively. Compared to the ED50 of other adenosine antagonists and dopamine agonist drugs, istradefylline is over 10 times as potent in these models. Istradefylline also ameliorated the hypolocomotion (minimum effective dose; 0.16 mg/kg) induced by nigral dopaminergic dysfunction with MPTP or reserpine treatment. Combined administrations of subthreshold doses of istradefylline and L-dopa (50 mg/kg, PO) exerted prominent effects on haloperidol-induced and reserpine-induced catalepsy, suggesting that there may be a synergism between the adenosine A2AR antagonist istradefylline and dopaminergic agents [8]. Istradefylline (3.3 mg/kg, i.p.) treatment before a single dose of MPTP attenuates the partial dopamine and DOPAC depletions measured in striata 1 week later [9]. Oral administration of istradefylline protected against the loss of nigral dopaminergic neuronal cells induced by 6-hydroxydopamine in rats. It also prevented the functional loss of dopaminergic nerve terminals in the striatum and the ensuing gliosis caused by MPTP in mice [10].
United States, New Jersey
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Kyowa Pharmaceutical Inc.
Princeton, New Jersey, United States, 08540
Kyowa Pharmaceutical
Princeton, New Jersey, United States, 08540 收起 <<
United States, Florida
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Orlando Clinical Research Center
Orlando, Florida, United States, 32908
United States, Tennessee
Noccr/Vrg
Knoxville, Tennessee, United States, 37920 收起 <<
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