RTIOX-276 is an

orexin antagonist An orexin receptor antagonist, or orexin antagonist, is a drug that inhibits the effect of orexin by acting as a receptor antagonist of one or both of the orexin receptors, Hypocretin (orexin) receptor 1, OX1 and Hypocretin (orexin) receptor 2, OX2. ...

. RTIOX-276 binds selectively to the orexin 1 receptor (K_E = 8.5nM) and lacks significant

affinity Affinity may refer to: Commerce, finance and law * Affinity (law), kinship by marriage * Affinity analysis, a market research and business management technique * Affinity Credit Union, a Saskatchewan-based credit union * Affinity Equity Par ...

for the orexin 2 receptor (K_E = > 10,000nM). RTIOX-276 may have therapeutic utility for the treatment of

cocaine addiction Cocaine dependence is a neurological disorder that is characterized by withdrawal symptoms upon cessation from cocaine use. It also often coincides with cocaine addiction which is a biopsychosocial disorder characterized by persistent use of coc ...

. In

conditioned place preference Conditioned place preference (CPP) is a form of Pavlovian conditioning used to measure the motivational effects of objects or experiences. This motivation comes from the pleasurable aspect of the experience, so that the brain can be reminded of th ...

studies, RTIOX-276 attenuated the development of place preference in mice exposed to

cocaine Cocaine (from , from , ultimately from Quechuan languages, Quechua: ''kúka'') is a central nervous system (CNS) stimulant mainly recreational drug use, used recreationally for its euphoria, euphoric effects. It is primarily obtained from t ...

References

Amides Benzylisoquinolines Orexin antagonists 3-Pyridyl compounds {{Sedative-stub