title: Thioxanthene-derived analogs as sigma(1) receptor ligands.
abstract: An investigation of the structure-affinity relationships for the binding of thioxanthene-related structures indicates that an intact thioxanthene ring is not required for binding at sigma(1) receptors, and that with the appropriate structural modifications, affinity can be enhanced to the subnanomolar level. Certain of the analogs displayed sigma(1)-fold selectivity for sigma(1) versus sigma(2) receptors.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, PO Box 980540, Richmond, VA 23298-0540, USA. glennon@hsc.vcu.edu
authors.forename: Richard A
authors.initials: RA
authors.lastname: Glennon
authors.forename: Abd M
authors.initials: AM
authors.lastname: Ismaiel
authors.forename: Seth
authors.initials: S
authors.lastname: Ablordeppey
authors.forename: Mahmoud
authors.initials: M
authors.lastname: El-Ashmawy
authors.forename: James B
authors.initials: JB
authors.lastname: Fisher
mesh_terms: D008024:Ligands; D017480:Receptors, sigma / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013892:Thioxanthenes / Q000737:chemistry / Q000378:metabolism*
chemical_list: D008024:Ligands; D017480:Receptors, sigma; D013892:Thioxanthenes