Abstract: Dopamine D3 receptor 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 D3 receptor affinity and selectivity, as well as water solubility, is achieved. A series of linking-chain derivatives are disclosed wherein functionality such as OH, OAc, and cis or trans-cyclopropyl groups have been introduced into the linking chain. In general, these modifications are well tolerated at D3 receptors and achieve high selectivity over D2 and D4 receptors.
Type:
Application
Filed:
April 30, 2014
Publication date:
October 2, 2014
Applicants:
The United States of America, as Represented by the Secretary, Department of Health and Human Serv, THE UNIVERSITY OF NORTH TEXAS HEALTH SCIENCE AT FORT WORTH
Inventors:
Amy Hauck Newman, Peter Grundt, George C. Cyriac, Robert Luedtke, Jianjing Cao