title: Synthesis and structure-activity relationship studies of conformationally flexible tetrahydroisoquinolinyl triazole carboxamide and triazole substituted benzamide analogues as σ2 receptor ligands.
abstract: Two novel classes of compounds targeting the sigma-2 (σ2) receptor were synthesized, and their bioactivities to binding σ1 and σ2 receptors were measured. Four novel triazole carboxamide analogues, 24d, 24e, 24f, and 39c, demonstrated high affinity and selectivity for the σ2 receptor. These data suggest (11)C-labeled versions of these compounds may be potential σ2-selective radiotracers for imaging the proliferative status of solid tumors.
authors.affiliation: Department of Radiology, Washington University School of Medicine , St. Louis, Missouri 63110, United States.
authors.forename: Suping
authors.initials: S
authors.lastname: Bai
authors.forename: Shihong
authors.initials: S
authors.lastname: Li
authors.forename: Jinbin
authors.initials: J
authors.lastname: Xu
authors.forename: Xin
authors.initials: X
authors.lastname: Peng
authors.forename: Kiran
authors.initials: K
authors.lastname: Sai
authors.forename: Wenhua
authors.initials: W
authors.lastname: Chu
authors.forename: Zhude
authors.initials: Z
authors.lastname: Tu
authors.forename: Chenbo
authors.initials: C
authors.lastname: Zeng
authors.forename: Robert H
authors.initials: RH
authors.lastname: Mach
mesh_terms: D000818:Animals; D001549:Benzamides / Q000138:chemical synthesis* / Q000378:metabolism; D045744:Cell Line, Tumor; D006168:Guinea Pigs; D008024:Ligands; D051379:Mice; D008968:Molecular Conformation; D017480:Receptors, sigma / Q000037:antagonists & inhibitors / Q000378:metabolism*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000378:metabolism; D000097605:Sigma-1 Receptor
chemical_list: D001549:Benzamides; D008024:Ligands; D017480:Receptors, sigma; D014230:Triazoles; D000097605:Sigma-1 Receptor; C106107:sigma-2 receptor