title: Predicting the antinociceptive efficacy of σ(1) receptor ligands by a novel receptor fluorescence resonance energy transfer (FRET) based biosensor.
abstract: We have developed a novel methodology for monitoring the σ1 receptor activation switch in living cells. Our assay uncovered the intrinsic nature of σ1 receptor ligands by recording the ligand-mediated conformational changes of this chaperone protein. The change triggered by each ligand correlated well with its ability to attenuate formalin induced nociception in an animal model of pain. This tool may assist in predicting the antinociceptive efficacy of σ1 receptor ligands.
authors.affiliation: Unitat de Farmacologia, Departament Patologia i Terapèutica Experimental, Facultat de Medicina, IDIBELL, Universitat de Barcelona , L'Hospitalet de Llobregat, 08907 Barcelona, Spain.
authors.forename: Maricel
authors.initials: M
authors.lastname: Gómez-Soler
authors.forename: Víctor
authors.initials: V
authors.lastname: Fernández-Dueñas
authors.forename: Enrique
authors.initials: E
authors.lastname: Portillo-Salido
authors.forename: Pilar
authors.initials: P
authors.lastname: Pérez
authors.forename: Daniel
authors.initials: D
authors.lastname: Zamanillo
authors.forename: José Miguel
authors.initials: JM
authors.lastname: Vela
authors.forename: Javier
authors.initials: J
authors.lastname: Burgueño
authors.forename: Francisco
authors.initials: F
authors.lastname: Ciruela
mesh_terms: D000700:Analgesics / Q000494:pharmacology*; D000818:Animals; D015374:Biosensing Techniques / Q000379:methods*; D031541:Fluorescence Resonance Energy Transfer / Q000379:methods*; D008024:Ligands; D051379:Mice; D017480:Receptors, sigma / Q000737:chemistry / Q000187:drug effects*; D000097605:Sigma-1 Receptor
chemical_list: D000700:Analgesics; D008024:Ligands; D017480:Receptors, sigma; D000097605:Sigma-1 Receptor