Preladenant

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).¹ It is selective for A_2A receptors over A₁, A_2B, and A₃ 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 (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.²

WARNING This product is not for human or veterinary use.

1. Neustadt, B.R., Hao, J., Lindo, N., et al. Potent, selective, and orally active adenosine A_2A receptor antagonists: Arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines. Bioorg. Med. Chem. Lett. 17(5), 1376-1380 (2007).

2. Pinna, A., Kin, W., Costa, G., et al. Antidyskinetic effect of A_2A and 5HT1A/1B receptor ligands in two animal models of Parkinson’s disease. Mov. Disord. 31(4), 501-511 (2016).