Using an implantable pump system to deliver drugs and sample cerebrospinal fluid (CSF), we assessed rostral redistribution and systemic uptake after intrathecal bolus injection and steady-state infusion of morphine sulfate and the opioid peptide ~A l a ~-~L e u ~-e n k e p h a l i n (DADL) in two pa
Synthesis of [D-Ala2, D-Leu5]enkephalin tritiated in the 2,6-positions of tyrosine
β Scribed by Hiroshi Hasegawa; Yoshihiko Shinohara; Shigeo Baba
- Publisher
- John Wiley and Sons
- Year
- 1996
- Tongue
- French
- Weight
- 351 KB
- Volume
- 38
- Category
- Article
- ISSN
- 0022-2135
No coin nor oath required. For personal study only.
β¦ Synopsis
D-Ma2, D-Leu51Enkephalin (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-Tyrl]DADLE, was performed by solid phase synthesis using F'moc strategy.
The peptide was tritiated catalytically to yield [2,6-3H-Tyrl] 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.
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Boc-Tyr-D-Ala-Gly was prepared by catalytic tritiation of protected, iodinated tripeptide. The protected tritiated tripeptide and the Phe-Leu-CH2C1 dipeptide were condensed by the mixed anhydride method. The p r o - 3 " tecting group was removed by HC1-methanol. The /JH/-DALECK had a specific activi
## Abstract As a study preliminary to attempts at photoaffinity and cooperative affinity labelling of cells and cell membrane vesicles bearing opiate receptors, the title compounds were prepared and tested by rat brain membrane binding assays and by a modified guineaβpig ileum bioβassay. The potenc
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