3 H]-Labelled 4- [ethyl[2,5,6-trimethyl-7-(2,4,6-trimethylphenyl)pyrrolo[2,3-d]pyrimidin-4-yl]amino]-2,3-[ 3 H]-butan-1-ol (3b) was prepared as a novel non-peptidic radiolabelled high affinity antagonist of the corticotropin-releasing hormone type 1 receptor (CRHR 1 ) that could be useful as a more
✦ LIBER ✦
[4-Amino-D-phenylalanine6]luliberin. A biologically active abalog of the luteinizing hormone-releasing factor suitable for affinity labeling
✍ Scribed by Constantinos Sakarellos; Bernard Donzel; Murray Goodman
- Book ID
- 101717292
- Publisher
- Wiley (John Wiley & Sons)
- Year
- 1976
- Tongue
- English
- Weight
- 349 KB
- Volume
- 15
- Category
- Article
- ISSN
- 0006-3525
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✦ Synopsis
Abstract
The syntheis of [4‐amino‐D‐phenylalanine^6^]luliberin by the solid‐phase method is described. The analog was found to be ten times more potent than luliberin. Some possibilities for the easy derivatization of the 4‐amino‐phenylalanyl residue into addinity labels suitable for the study of hormone‐receptor interations are considered. The preparation of N^α^‐t‐butyloxycarbonyl‐4‐(benzyloxycarbonylamino)‐D‐phenylalanine, one of the key intermediates used in the synthesis of this luliberin analog, is also reported.
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