Tritium labelling of highly selective probes for δ‐opioid receptors: [3H] Tyr‐D‐Ser(O‐t‐Bu)‐Gly‐Phe‐Leu‐Thr(DSTBULET) and [3H]Tyr‐D‐Ser(O‐t‐Bu)‐Gly‐Phe‐Leu‐Thr(O‐t‐Bu)(BUBU)
- 1 August 1990
- journal article
- research article
- Published by Wiley in Journal of Labelled Compounds and Radiopharmaceuticals
- Vol. 28 (8) , 867-876
- https://doi.org/10.1002/jlcr.2580280802
Abstract
The introduction of bulky residue (s) in linear enkephalin‐related hexapeptides represents a new approach in the design of selective probes for δ‐opioid receptors, displaying the appropriate criteria to investigate biological and pharmacological properties of the assumed binding site (δ) of endogenous enkephalins. The selectivities and high affinities of Tyr‐D‐Ser(O‐t‐Bu)‐Gly‐Phe‐Leu‐Thr(DSTBULET) and especially Tyr‐D‐Ser(O‐T‐Bu)‐Gly‐Phe‐Leu‐Thr(O‐t‐Bu) (BUBU) associated with a satisfactory resistance to peptidases, make them the most suitable δ–probes reported to date. In the present paper, we report the synthesis of DSTBULET and BUBU under tritiated forms with high specific radioactivities. These radio‐labelled probes will enable extensive in vitro and in vivo investigations of δ–opioid receptors properties to be carried out.Keywords
This publication has 17 references indexed in Scilit:
- Use of μ and δ opioid peptides of various selectivity gives further evidence of specific involvement of μ opioid receptors in supraspinal analgesia (tail-flick test)European Journal of Pharmacology, 1987
- Opioid receptor subtypes in the rat spinal cord: electrophysiological studies with μ- and δ-opioid receptor agonists in the control of nociceptionBrain Research, 1987
- Different effects of μ and δ opiate agonists on respirationEuropean Journal of Pharmacology, 1984
- Bis-penicillamine enkephalins possess highly improved specificity toward delta opioid receptors.Proceedings of the National Academy of Sciences, 1983
- Tritium labelling of enkephalin analogs : Tyr‐D‐Ala‐Gly‐NH‐CH(CH3)‐CH2‐CH(CH3)2 (trimu 4), Tyr‐D‐Ser‐Gly‐Phe‐Leu‐Thr (DSLET), Tyr‐D‐Thr‐Gly‐Phe‐Leu‐Thr (DTLET), μ and δ opiate‐receptors specific ligandsJournal of Labelled Compounds and Radiopharmaceuticals, 1983
- Deltakephalin, Tyr-D-Thr-Gly-Phe-Leu-Thr: A new highly potent and fully specific agonist for opiate δ-receptorsBiochemical and Biophysical Research Communications, 1983
- Improved assays for the assessment of ϰ- and δ-properties of opioid ligandsEuropean Journal of Pharmacology, 1982
- Dynorphin1–8 and dynorphin1–9 are ligands for the κ-subtype of opiate receptorNature, 1982
- D‐Tyr—Ser—Gly—Phe—Leu—Thr, a highly preferential ligand for δ‐opiate receptorsFEBS Letters, 1980
- Endogenous opioid peptides: multiple agonists and receptorsNature, 1977