Preladenant

Preladenant is an orally bioavailable antagonist of the adenosine A2A receptor (Kis = 1.1 and 2.5 nM for human and rat receptors, respectively). 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 (Cay-17126). It inhibits catalepsy induced by haloperidol (Cay-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 (Cay-13248) when used in combination with eltoprazine (Cay-18428) in a 6-OHDA rat lesion model of Parkinson's disease dyskinesia.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. CAS Number: 377727-87-2. Synonyms: SCH 420814. Molecular Formula: C25H29N9O3. Formula Weight: 503.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: slightly soluble, Ethanol: slightly soluble. lambdamax: 259 nm. SMILES: COCCOC1=CC=C(N2CCN(CCN3N=CC4=C3N=C(N)N5C4=NC(C6=CC=CO6)=N5)CC2)C=C1. InChi Code: InChI=1S/C25H29N9O3/c1-35-15-16-36-19-6-4-18(5-7-19)32-11-8-31(9-12-32)10-13-33-23-20(17-27-33)24-28-22(21-3-2-14-37-21)30-34(24)25(26)29-23/h2-7,14,17H,8-13,15-16H2,1H3,(H2,26,29). InChi Key: DTYWJKSSUANMHD-UHFFFAOYSA-N.