131124-60-2Relevant articles and documents
Synthesis of 2>Leu-enkephalin and 2,D-Leu5>Leu-enkephalin with High Specific Tritiated Activity in the Leucine Residue
Hasegawa, Hiroshi,Shinohara, Yoshihiko,Baba, Shigeo
, p. 2641 - 2644 (2007/10/02)
2>Leu-enkephalin and 2,D-Leu5>Leu-enkephalin (DADLE) labelled with tritium in the leucine residue have been prepared.Synthesis of the precursor peptides, 2,4,5-didehydro-L-Leu5>Leu-enkephalin and 2,4,5-didehydro-D-Leu5>Leu-enkephalin, was carried out by solid-phase synthesis using Fmoc amino acid derivatives, followed by diastereoisomeric separation on HPLC.These peptides were tritiated catalytically to yield DALE with a specific activity of 5.35 TBq mmol-1 and DADLE with that of 5.43 TBq mmol-1, respectively.The distribution of tritium label was investigated by HPLC with a radioisotopic detector following acidic hydrolysis, which confirmed that the tritium label in both labelled peptides was exclusively located at the leucine residue.