Abstract：
:The recently discovered highly specific delta opioid antagonist H-Tyr-Tic-Phe-Phe-OH (TIPP) was radiolabelled by catalytic tritiation of its precursor [Tyr (3', 5'-I2)1]TIPP. The tritiated ligand labelled rat brain membrane binding sites with a Kd value of 0.64 nM and a Bmax of 82 fmol/mg protein. Binding competition experiments with various unlabelled mu-, delta- and kappa-opioid receptor ligands resulted in mu/delta and kappa/delta selectivity ratios of 600 and 9100, respectively, and thus confirmed the previously established high delta specificity of TIPP. Because of its high delta receptor affinity, extraordinary delta selectivity and low non-specific binding, [3H]TIPP represents an excellent new radioligand for the study of delta opioid receptor interactions.
journal_name
Life Scijournal_title
Life sciencesauthors
Nevin ST,Toth G,Nguyen TM,Schiller PW,Borsodi Adoi
10.1016/0024-3205(93)90649-nsubject
Has Abstractpub_date
1993-01-01 00:00:00pages
PL57-62issue
5eissn
0024-3205issn
1879-0631pii
0024-3205(93)90649-Njournal_volume
53pub_type
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