An adenosine A2A receptor antagonist (Kis = 1.1 and 2.5 nM for human and rat receptors

Preladenant – 1 mg

Brand:
Cayman
CAS:
377727-87-2
Storage:
-20
UN-No:
Non-Hazardous - /

Preladenant is an orally bioavailable antagonist of the adenosine A2A receptor (Kis = 1.1 and 2.5 nM for human and rat receptors, respectively).{40675} It is selective for A2A receptors over A1, A2B, and A3 receptors (Kis = >1,000, >1,700, and >1,000 nM, respectively) as well as a panel of 59 receptors, enzymes, and ion channels. Preladenant inhibits adenylate cyclase activity (Kbs = 1.3 and 0.7 nM for human and rat receptors, respectively) induced by the A2A receptor agonist CGS 21680 (Item No. 17126). It inhibits catalepsy induced by haloperidol (Item No. 12014) in rats by 77 and 70% after 1 and 4 hours, respectively, when administered at a dose of 1 mg/kg. Preladenant also increases the efficacy of L-DOPA (Item No. 13248) when used in combination with eltoprazine (Item No. 18428) in a 6-OHDA rat lesion model of Parkinson’s disease dyskinesia.{40676}  

 

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Description

An adenosine A2A receptor antagonist (Kis = 1.1 and 2.5 nM for human and rat receptors, respectively); selective for A2A receptors over A1, A2B, and A3 receptors, with Ki values greater than 1,000 nM, and a panel of receptors enzymes and ion channels; inhibits A2A receptor agonist-induced adenylate cyclase activity (Kbs = 1.3 and 0.7 nM for human and rat receptors, respectively); inhibits catalepsy induced by haloperidol in rats by 77 and 70% after 1 and 4 hours, respectively (1 mg/kg); increases the efficacy of L-DOPA when used in combination with eltoprazine

Formal name: 2-(2-furanyl)-7-[2-[4-[4-(2-methoxyethoxy)phenyl]-1-piperazinyl]ethyl]-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine

Synonyms:  SCH 420814

Molecular weight: 503.6

CAS: 377727-87-2

Purity: ≥98%

Formulation: A crystalline solid

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

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