Home GPCR & G Protein Adenosine Receptor antagonist Istradefylline For research use only.

Istradefylline

Synonyms: KW-6002

Istradefylline (KW-6002) is a selective adenosine A2A receptor (A2AR) antagonist with Ki of 2.2 nM. Phase 3.

Istradefylline Chemical Structure

Istradefylline Chemical Structure

CAS No. 155270-99-8

Purity & Quality Control

Batch: S279001 DMSO]6 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.88%
99.88

Istradefylline Related Products

Biological Activity

Description Istradefylline (KW-6002) 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
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
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 LevoDOPA (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/LevoDOPA) in combination with SKF80723 (1 mg/kg, ip), quinpirole (0.06 mg/kg ip), or LevoDOPA (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]
Animal Research Animal Models Common marmosets (Callithrix jacchus) with MPTP treatment
Dosages 10 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05885360 Active not recruiting
Parkinson Disease|Tremor
Georgetown University|Kyowa Kirin Inc.
 January 20 2023 Phase 4
NCT02610231 Completed
Idiopathic Parkinson''s Disease
Kyowa Kirin Co. Ltd.|Kyowa Hakko Kirin Pharma Inc.
 December 2015 Phase 3
NCT02256033 Completed
Hepatic Impairment
Kyowa Kirin Co. Ltd.|Kyowa Hakko Kirin Pharma Inc.
 August 2014 Phase 1
NCT00455507 Completed
Parkinson''s Disease
Kyowa Kirin Co. Ltd.
 March 2007 Phase 2

Chemical Information & Solubility

Molecular Weight 384.43 Formula

C20H24N4O4
CAS No. 155270-99-8 SDF Download Istradefylline SDF
Smiles CCN1C2=C(C(=O)N(C1=O)CC)N(C(=N2)C=CC3=CC(=C(C=C3)OC)OC)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 6 mg/mL ( (15.6 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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