OX-201 is a selective agonist for OX2R with an EC50 of 8 nM. Pathological proteins produced by neurons are released into the interstitial fluid (ISF) in a neural activity-dependent manner and subsequently cleared from the brain via lymphatic pathways. The efflux of these proteins to the ISF correlates with the wakeful state of neurons. OX-201 can induce neuronal awakening and enhance the release of tau into the hippocampal ISF. While it does not alter hippocampal tau levels, OX-201 has potential applications in Alzheimers disease (AD) related to sleep/wake cycle disturbances.

OX1 receptor:8.1 μM (EC50), OX2 receptor:8 nM (EC50)