title: Solid-phase synthetic strategy and bioevaluation of a labeled delta-opioid receptor ligand Dmt-Tic-Lys for in vivo imaging.
abstract: A general solid-phase synthetic strategy is developed to prepare fluorescent and/or lanthanide-labeled derivatives of the delta-opioid receptor (deltaOR) ligand H-Dmt-Tic-Lys(R)-OH. The high delta-OR affinity (K(i) = 3 nM) and desirable in vivo characteristics of the Cy5 derivative 1 suggest its usefulness for structure-function studies and receptor localization and as a high-contrast noninvasive molecular marker for live imaging ex vivo or in vivo.
authors.affiliation: Department of Chemistry, BIO5 Institute, The University of Arizona, Tucson, Arizona 85721, USA.
authors.forename: Jatinder S
authors.initials: JS
authors.lastname: Josan
authors.forename: David L
authors.initials: DL
authors.lastname: Morse
authors.forename: Liping
authors.initials: L
authors.lastname: Xu
authors.forename: Maria
authors.initials: M
authors.lastname: Trissal
authors.forename: Brenda
authors.initials: B
authors.lastname: Baggett
authors.forename: Peg
authors.initials: P
authors.lastname: Davis
authors.forename: Josef
authors.initials: J
authors.lastname: Vagner
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Gillies
authors.forename: Victor J
authors.initials: VJ
authors.lastname: Hruby
mesh_terms: D000345:Affinity Labels; D000818:Animals; D002232:Carbocyanines / Q000737:chemistry; D003952:Diagnostic Imaging; D005456:Fluorescent Dyes / Q000737:chemistry; D007546:Isoquinolines / Q000138:chemical synthesis*; D008024:Ligands; D051379:Mice; D017465:Receptors, Opioid, delta / Q000737:chemistry / Q000378:metabolism*; D013237:Stereoisomerism
chemical_list: D000345:Affinity Labels; D002232:Carbocyanines; D005456:Fluorescent Dyes; D007546:Isoquinolines; D008024:Ligands; D017465:Receptors, Opioid, delta; C085321:cyanine dye 5