The United States of America, as Represented by the Secretary, Department of Health and Human Services

University of North Texas

Jianjing Cao

Amy Hauck Newman

Oluyomi M Okunola-Bakare

Peter Grundt

Robert R Luedtke

George C Cyriac

Robert Leudtke

Disclosed herein are bisarylmethylthioacetamides and bisarylmethylthioethylamines useful as inhibitors of monoamine transporters. The compounds are potent and/or selective inhibitors of dopamine (DA), serotonin (5-HT), and/or norepinephrine (NE) reuptake via their respective transporters, DAT, SERT and NET. Also disclosed are methods for eliciting a wake-promoting or cognitive or attention enhancing effect and for treating substance use disorders, attention deficit (hyperactivity) disorder, depressive disorders, bipolar disorder or other neuropsychiatric disorders sleep disorders or cognitive impairment using the compounds.

Potent and selective inhibitors of monoamine transporters; method of making; and use thereof

Dopamine Dreceptor antagonists and partial agonists are known to modulate the reinforcing and drug-seeking effects induced by cocaine and other abused substances. By introducing functionality into the butylamide linking chain of the 4-phenylpiperazine class of ligands, improved Dreceptor affinity and selectivity, as well as water solubility, is achieved. A series of linking-chain derivatives are disclosed wherein functionality such as OH or OAc groups have been introduced into the linking chain. In general, these modifications are well tolerated at Dreceptors and achieve high selectivity over Dand Dreceptors.

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Ellicott City, MD, United States of America

Jianjing Cao