title: Trifluoromethoxyl substituted phenylethylene diamines as high affinity sigma receptor ligands with potent anti-cocaine actions.
abstract: The phenylethylene diamines are a class of sigma receptor ligands with excellent selectivity over other biological systems and with anti-cocaine actions that involve antagonism of sigma1 receptors. In order to increase the potency of the aromatic methoxyl substituted analogues, trifluoromethoxyl groups were introduced to prevent metabolic demethylation. The para-substituted trifluoromethoxyl substituted analogues were shown to have increased sigma receptor affinity and represent the most potent anti-cocaine phenylethylene diamines yet described.
authors.affiliation: Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, MD 21201, USA.
authors.forename: Trudy A
authors.initials: TA
authors.lastname: Smith
authors.forename: Xiaowen
authors.initials: X
authors.lastname: Yang
authors.forename: Huifang
authors.initials: H
authors.lastname: Wu
authors.forename: Buddy
authors.initials: B
authors.lastname: Pouw
authors.forename: Rae R
authors.initials: RR
authors.lastname: Matsumoto
authors.forename: Andrew
authors.initials: A
authors.lastname: Coop
mesh_terms: D000818:Animals; D001921:Brain / Q000378:metabolism; D019970:Cocaine-Related Disorders / Q000188:drug therapy*; D003959:Diamines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008024:Ligands; D008297:Male; D051379:Mice; D010627:Phenethylamines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D017480:Receptors, sigma / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D003959:Diamines; D008024:Ligands; D010627:Phenethylamines; D017480:Receptors, sigma