Solid-phase synthetic strategy and bioevaluation of a labeled delta-opioid receptor ligand Dmt-Tic-Lys for in vivo imaging.
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.
Josan
Jatinder S
JS
Department of Chemistry, BIO5 Institute, The University of Arizona, Tucson, Arizona 85721, USA.
Morse
David L
DL
Xu
Liping
L
Trissal
Maria
M
Baggett
Brenda
B
Davis
Peg
P
Vagner
Josef
J
Gillies
Robert J
RJ
Hruby
Victor J
VJ
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
D000345:Affinity Labels; D002232:Carbocyanines; D005456:Fluorescent Dyes; D007546:Isoquinolines; D008024:Ligands; D017465:Receptors, Opioid, delta; C085321:cyanine dye 5