Istradefylline

Catalog No.S2790 Synonyms: KW-6002

Istradefylline Chemical Structure

Molecular Weight(MW): 384.43

Istradefylline is a selective adenosine A2A receptor (A2AR) antagonist with Ki of 2.2 nM. Phase 3.

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  • The effect of caffeine (CAF) and adenosine A1 and A2A receptor antagonists, DPCPX and KW 6002 (KW) on DA release induced by MDMA in the mouse striatum.KW (1.25 and 2.5 mg/kg) were injected simultaneously with MDMA 20 or 40 mg/kg as indicated with an arrow. Values are the mean ± SEM (n = 6–8 animals). *P < 0.0001 represents a significant difference in comparison to control group; “a” P < 0.0002 represents a significant difference in comparison to MDMA group (repeated measures ANOVA and Tukey’s post-hoc test)

    Neurotox Res, 2015, 27(3):229-45.. Istradefylline purchased from Selleck.

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Biological Activity

Description Istradefylline is a selective adenosine A2A receptor (A2AR) antagonist with Ki of 2.2 nM. Phase 3.
Targets
Adenosine A2A receptor [1]
2.2 nM(Ki)
In vitro

The affinity of Istradefylline for the A2AR is 70-fold greater than that for the A1 receptor with Ki of 2.2 nM versus 150 nM. [1] Exposure of primary rat striatal astrocytes to Istradefylline results in concentration-dependent abolition of bFGF induction of astrogliosis in vitro. [5] Binding affinities (Ki) of Istradefylline for A1 receptor, A2A receptor, and A3 receptor in human are >287 nM, 9.12 nM, and >681 nM, respectively, for A1 receptor and A2A receptor in rat 50.9 nM and 1.57 nM, respectively, and for A1 receptor and A2A receptor in mouse 105.02 nM and 1.87 nM, respectively. [6]

In vivo Istradefylline reverses CGS21680-induced and reserpine-induced catalepsy with ED50 of 0.05 mg/kg and 0.26 mg/kg, respectively. Istradefylline is over 10 times as potent in these models compared to other adenosine antagonists and dopamine agonist drugs. Administration of Istradefylline in combination with L-dopa (50 mg/kg) exerts prominent effects on haloperidol-induced and reserpine-induced catalepsy. [2] Oral administration of Istradefylline at 10 mg/kg to MPTP-treated common marmosets produces an increase in locomotor activity to approximately twice that of control and improves motor disability. Administration of Istradefylline (10 mg/kg, po, 90 minutes before SKF80723/quinpirole/L-DOPA) in combination with SKF80723 (1 mg/kg, ip), quinpirole (0.06 mg/kg ip), or L-DOPA (2.5 mg/kg po) produces a significant additive effect on locomotor activity and improvement of motor disability but not dyskinesia. [3] In the MPTP mice model, Istradefylline significantly attenuates striatal dopamine depletion under various conditions. Pretreatment with Istradefylline (3.3 mg/kg, i.p.) before a single dose of MPTP attenuates the partial dopamine and DOPAC depletions measured in striata 1 week later. [1] Oral administration of Istradefylline protects against the loss of nigral dopaminergic neuronal cells induced by 6-hydroxydopamine in rats, and prevents the functional loss of dopaminergic nerve terminals in the striatum and the ensuing gliosis caused by MPTP in mice. [4] Chronic Istradefylline treatment does not improve the reversal deficits in dopamine-depleted rats. [7] The tremulous jaw movements induced by pimozide are significantly reduced by co-administration of either Istradefylline or tropicamide. Pimozide-induced increases in ventrolateral striatal c-Fos expression are reduced by a behaviorally effective dose of Istradefylline, in contrast to tropicamide by which c-Fos expression in pimozide-treated rats is actually increased. [8]

Protocol

Animal Research:[2]
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  • Animal Models: Common marmosets (Callithrix jacchus) with MPTP treatment
  • Formulation: Suspended in 0.3% Tween-80 and 10% sucrose solution
  • Dosages: 10 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 6 mg/mL (15.6 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 384.43
Formula

C20H24N4O4

CAS No. 155270-99-8
Storage powder
Synonyms KW-6002

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02609477 Completed Drug Abuse Kyowa Hakko Kirin Pharma, Inc.|Kyowa Hakko Kirin Co., Ltd|Kyowa Kirin Pharmaceutical Development, Inc. January 2016 Phase 1
NCT02610231 Active, not recruiting Idiopathic Parkinsons Disease Kyowa Hakko Kirin Pharma, Inc.|Kyowa Hakko Kirin Co., Ltd|Kyowa Kirin Pharmaceutical Development, Inc. December 2015 Phase 3
NCT02256033 Completed Hepatic Impairment Kyowa Hakko Kirin Pharma, Inc.|Kyowa Kirin Pharmaceutical Development, Inc. August 2014 Phase 1
NCT02174250 Completed Parkinsons Disease Kyowa Hakko Kirin Pharma, Inc.|Kyowa Kirin Pharmaceutical Development, Inc. June 2014 Phase 1
NCT01968031 Completed Idiopathic Parkinsons Disease Kyowa Hakko Kirin Pharma, Inc.|Kyowa Hakko Kirin Co., Ltd|Kyowa Kirin Pharmaceutical Development, Inc. October 2013 Phase 3
NCT00957203 Completed Parkinsons Disease Kyowa Hakko Kirin Co., Ltd October 2009 Phase 3

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