Synthesis of [D-Ala2, D-Leu5]enkephalin tritiated in the 2,6-positions of tyrosine
作者:Hiroshi Hasegawa、Yoshihiko Shinohara、Shigeo Baba
DOI:10.1002/(sici)1099-1344(199609)38:9<825::aid-jlcr907>3.0.co;2-a
日期:1996.9
[D-Ala(2), D-Leu(5)]Enkephalin (DADLE) labelled with tritium in the 2,6-positions of N-terminus tyrosine residue has been prepared. Synthesis of the precursor peptide, [2,6-dibromo-Tyr(1)]DADLE, was performed by solid phase synthesis using Fmoc strategy. The peptide was tritiated catalytically to yield [2,6-H-3-Tyr(1)]DADLE with a specific radioactivity of 1.61 TBq/mmol. The distribution of the tritium was investigated by HPLC with radioisotope detection following hydrolysis with aminopeptidase M, and confirmed that the label was entirely located at the tyrosine residue.