A library of novel compounds that selectively bind the dopamine D3 receptor have been designed and characterized extensively. In vivo rodent studies indicate selected lead molecules may be useful to treat drug addiction/dependence.
Scientists at the National Institute on Drug Abuse (NIDA) have developed novel dopamine D3 receptor (D3R) agonists with high affinity and selectivity. Two lead compounds, 53 and eutomer 53a, have demonstrated significantly higher D3R binding selectivity than reference compounds. Moreover, 53 and 53a showed metabolic stability in liver microsomes, which is favorable for the future use of these compounds as therapeutic agents for diseases related to dopamine system dysregulation such as Parkinson’s Disease and Restless Legs Syndrome. Researchers at NIDA seek licensing and/or co-development research collaborations for the use of these D3R agonists as molecular tools for the study of D3R physiology and as potential therapeutics to treat neurological and neuropsychiatric disorders.