Rapastinel

Rapastinel (5-10 mg/kg; intravenous injection, once daily for 3 consecutive days) exerts rapid antidepressant-like effects in mice with CUS-induced depression, reverses behavioral deficits, and normalizes the ERK/mTOR/VGF/BDNF signaling pathway in the hippocampus and prefrontal cortex (PFC); in contrast, Rapastinel (0.5 mg/kg; intravenous injection, once daily for 3 consecutive days) shows no activity^[1].
A single intravenous administration of Rapastinel (3 mg/kg) produces sustained antidepressant-like and anxiolytic-like effects in male Sprague-Dawley rats for at least 1 week, as evidenced by significant changes in ultrasonic vocalizations, time spent in the central zone of the open field test, and immobility time in the Porsolt forced swim test. It also induces sustained cognitive-enhancing effects, as reflected by improved behavioral performance of rats in spontaneous alternation, positive affective learning, Morris water maze, and contextual fear extinction tests^[3].
Rapastinel (1 mg/kg; subcutaneous injection; twice daily; administered for 3 or 5 days) reverses subchronic Phencyclidine-induced novel object recognition (NOR) impairment for at least 9 or 10 weeks, respectively, whereas Rapastinel (1 mg/kg; subcutaneous injection; 30 minutes in advance; single dose) only transiently reverses NOR function when the test interval is 24 hours^[4].
Rapastinel (10-30 mg/kg; subcutaneous injection; single administration) produces rapid and sustained antidepressant-like effects in rats, corresponding to concentrations of approximately 30 nM and ~100 nM in the medial prefrontal cortex (mPFC), respectively^[5].