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Atypical Inhibitors of Monoamine Transporters; Method of Making; and Use Thereof

The technology is a series of modafinil analogues that bind with moderate to high affinity to the dopamine (DA) transporter (DAT). Some compounds also have affinity for the serotonin (5-HT) transporter (SERT) and/or sigma-1 receptor. The compounds retain the desired dopamine transporter affinity with greater metabolic stability over previously described unsubstituted piperazine ring analogues. Importantly, these compounds have no predicted addictive liability. Also disclosed are methods for treating substance use disorders as well as other neuropsychiatric disorders such as ADHD, depression, narcolepsy, and cognitive impairment. Researchers at the National Institute on Drug Abuse (NIDA) seek licensing and/or co-development research collaborations for further development and commercialization of the compounds.

Dopamine D3 Receptor Agonist Compounds, Methods of Preparation, Intermediates Thereof, and their Methods of Use

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.