PW0787 (C09-1163-833)

PW0787 is a potent, selective, orally active, and brain-penetrant GPR52 agonist ( EC 50 =135 nM). PW0787 suppresses psychostimulant behaviorIn VivoPW0787 (0.3, 1, 3, or 10 mg/kg; IP) displays antipsychotic-like activity by significantly inhibiting amphetamine-induced hyperlocomotor behavior in mice . PW0787 is evaluated in rats after a single dose of 20 mg/kg by oral (PO) or 10 mg/kg by intravenous (IV) administration. PW0787 has excellent plasma exposure after PO (AUC 0-inf = 13,749 ng•h/mL) and IV dosing (AUC 0-inf =9030 ng•h/mL), as well as high maximum serum concentration following PO (C max =3407 ng/mL) and IV administration (C max =6726 ng/mL). Additionally, PW0787 displays good volume of plasma distribution (V ss =1.5 L/kg) and acceptable plasma clearance (CL=1.1 L/h/kg) after 10 mg/kg IV. Excellent oral bioavailability (F) with the value of 76% is observed . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Naïve male C57/BL6 mice weighing between 24 and 31 g Dosage: 0.3, 1, 3, or 10 mg/kg (dissolved in 0.9% saline containing 20% HP-β-CD with a final pH of the solution adjusted to 7.4) Administration: IP Result: Suppressed amphetamine (AMPH)-induced horizontal activity at both 3 mg/kg and 10 mg/kg doses.Form:SolidIC50& Target:EC50: 135 nM (GPR52). Specification: 0.99 Molecular Formula: C23H20F4N4O2 Molecular Weight: 460.4 PubChem CID: 155977949 Isomeric SMILES: C1CN(C2=CC=CC(=C21)C(=O)NCCO)C3=NC=NC(=C3)CC4=CC(=CC(=C4)F)C(F)(F)F