An A2A receptor antagonist (Ki = 2.2 nM in a radioligand binding assay); inhibits haloperidol-induced catalepsy (ED50 = 0.23 mg/kg in rats); alleviates postural defects in a dose-dependent manner without inducing dyskinesias or hyperactivity in an MPTP-induced marmoset model of Parkinson's disease; decreases bradykinesias induced by L-DOPA and improves attentional and working memory deficits in an MPTP-induced macaque model of Parkinson's disease

Istradefylline – 25 mg

Brand:
Cayman
CAS:
155270-99-8
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Istradefylline is an adenosine receptor 2A (A2A) antagonist (Ki = 2.2 nM in a radioligand binding assay).{37122} In vivo, istradefylline inhibits catalepsy induced by haloperidol (Item No. 12014) with an ED50 value of 0.23 mg/kg in rats. Oral administration of istradefylline alleviates postural defects in a dose-dependent manner without inducing dyskinesias or hyperactivity in an MPTP-induced marmoset model of Parkinson’s disease.{37123} It also decreases bradykinesias induced by L-DOPA (Item No. 13248) and improves attentional and working memory deficits in an MPTP-induced macaque model of Parkinson’s disease.{37124} Formulations containing istradefylline are used to extend on-time in Parkinson’s disease patients experiencing motor fluctuations.  

 

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Description

An A2A receptor antagonist (Ki = 2.2 nM in a radioligand binding assay); inhibits haloperidol-induced catalepsy (ED50 = 0.23 mg/kg in rats); alleviates postural defects in a dose-dependent manner without inducing dyskinesias or hyperactivity in an MPTP-induced marmoset model of Parkinson’s disease; decreases bradykinesias induced by L-DOPA and improves attentional and working memory deficits in an MPTP-induced macaque model of Parkinson’s disease

Formal name: 8-[(1E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-3,7-dihydro-7-methyl-1H-purine-2,6-dione

Synonyms:  KW 6002

Molecular weight: 384.4

CAS: 155270-99-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory||Research Area|Neuroscience|Neurodegenerative Disorders|Parkinson’s Disease

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