Synthesis of [3H] tyr-D-thr-gly-phe(pN3)-leu-thr an irreversible photoaffinity probe for the opioid δ receptors
✍ Scribed by G. Gacel; E. Fellion; B. B. Roques; R. Genet; J. J. Morgat; P. Fromageot
- Publisher
- John Wiley and Sons
- Year
- 1987
- Tongue
- French
- Weight
- 388 KB
- Volume
- 24
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
3
In a previous work, the synthesis of [ HI Tyr-D-Thr-Gly-Phe-Leu-Thr (DTLET), a highly selective probe for 6 opioid receptors has been described. More recently, Az-DTLET (Tyr-D-Thr-Cly-Phe (pN 1-Leu-Thr) has been shown to be a specific and irreversible photoaffinity ligand for 6 opioid sites. In the present paper, we reported the synthesis of the 3,5 dibromotyrosyl 4' -aminO-3' ,5' di iodophenylalanyl precursor of 13H] Az-DTLET. Reductive tritiation by exchange with 3H2 followed by the introduction of the azido group leads to the labelled azido analog of enkephalin with specific activity of 50 Ci/mmole. This compound is now used to characterize the subunits of opioid 6 receptors and to visualize these targets in the brain by electron microscopy.