LSN2814617 is an orally active, potent, brain-penetrant, and selective mGlu 5 (metabotropic glutamate 5) positive allosteric modulator (PAM), with EC 50 values of 52 nM (Human mGlu5) and 42 nM (rat mGlu5). In vivo EEG studies demonstrated that LSN2463359 has marked wake-promoting properties but little in the way of rebound hypersomnolence. LSN2814617 can be used for schizophrenia research [1].

LSN2814617 (1nM-10 μM) fails to elicit responses alone in rat cortical neurons, and causes a concentration-dependent increase in the [Ca2+]i response in AV12 cells [1].

LSN2814617 (0.3-60 mg/kg, Orally, once) shows significant unbound brain exposure and dose-dependent occupancy of the mGlu5 receptor [1]. LSN2814617 (0-10 mg/kg, Orally, once) significantly modulates amphetamine-induced locomotor hyperactivity [1]. LSN2814617 (0-3 mg/kg, Orally, once) significantly increase wakefulness [1]. Animal Model: Male Lister Hooded rats (180-250 g, four to eight per cage) [1] Dosage: 0, 2.5, 5, and 10 mg/kg Administration: Orally, once, 60 min before amphetamine Result: Significantly modulated amphetamine hyperactivity, although a trend level decrease in hyperactivity was observed for the highest dose. At the end of the test session, from 75 to 120 min, the 10 mg/kg dose of LSN2814617 significantly increased amphetamine-induced hyperactivity. Animal Model: Adult male Wistar rats (approximately 270 g) [1] Dosage: 0, 0.3, 1, and 3 mg/kg Administration: Orally, once Result: Displayed dose-dependently increase in wakefulness immediately following oral administration; Produced 234 ± 16 min of increased wake for over 7 h in the case of 3 mg/kg. Produced dose-dependent reductions in both NREM and REM sleep.