Highly selective fluorescent analogue of the potent delta-opioid receptor antagonist Dmt-Tic.
A fluorescent tripeptide probe derived by coupling fluorescein to H-Dmt-Tic-Glu-NH2 was developed to interact with delta-opioid receptors with high affinity (Ki = 0.035 nM) and selectivity (Ki(mu)/Ki(delta) = 4371). It acts as an irreversible delta-opioid receptor antagonist, and binding to NG108-15 cells is blocked by the standard nonpeptidic delta-opioid receptor antagonist naltrindole. This probe should prove useful in the study of the distribution of delta-opioid receptors in tissues and the internalization of opioid peptides during signal transduction.
Balboni
Gianfranco
G
Department of Toxicology, University of Cagliary, I-09126, Cagliary, Italy.
Salvadori
Severo
S
Dal Piaz
Alessandro
A
Bortolotti
Fabrizio
F
Argazzi
Roberto
R
Negri
Lucia
L
Lattanzi
Roberta
R
Bryant
Sharon D
SD
Jinsmaa
Yunden
Y
Lazarus
Lawrence H
LH
D000818:Animals; D001921:Brain / Q000378:metabolism / Q000648:ultrastructure; D002460:Cell Line; D004151:Dipeptides / Q000737:chemistry*; D004558:Electric Stimulation; D005456:Fluorescent Dyes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects / Q000502:physiology; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects / Q000502:physiology; D011869:Radioligand Assay; D051381:Rats; D017465:Receptors, Opioid, delta / Q000037:antagonists & inhibitors*; D013574:Synaptosomes / Q000187:drug effects / Q000378:metabolism; D044005:Tetrahydroisoquinolines / Q000737:chemistry*; D014649:Vas Deferens / Q000187:drug effects / Q000502:physiology
C446951:2',6'-dimethyltyrosyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid; D004151:Dipeptides; D005456:Fluorescent Dyes; D017465:Receptors, Opioid, delta; D044005:Tetrahydroisoquinolines