Description
Preladenant is an orally bioavailable antagonist of the adenosine A
2A receptor (K
is = 1.1 and 2.5 nM for human and rat receptors, respectively). It is selective for A
2A receptors over A
1, A
2B, and A
3 receptors (K
is = >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 (K
bs = 1.3 and 0.7 nM for human and rat receptors, respectively) induced by the A
2A receptor agonist CGS 21680 . It inhibits catalepsy induced by haloperidol 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 when used in combination with eltoprazine in a 6-OHDA rat lesion model of Parkinson’s disease dyskinesia.
References
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