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Tritiation of Peptides to High Specific Radioactivity. Part 1. Synthesis and Biological Properties of [13-(3H4)Norvaline]-α-MSH and of [2,23-Bis((3H2)tyrosine)]ACTH(1–24)

✍ Scribed by Alex N. Eberle; Albert Zeller


Publisher
John Wiley and Sons
Year
1985
Tongue
German
Weight
894 KB
Volume
68
Category
Article
ISSN
0018-019X

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✦ Synopsis


Radium-Chemie. CH-9053 Teufen

Dedicated to Professor Max Brenner, Basel, on the occasion of his 70th birthday (29.VII.85) a-MSH and ACTH(1-24) were tritiated to high specific radioactivity ( > 100 Ci/mmol) using a new tritiation apparatus with which the tritiation reaction can be performed at slightly elevated pressure. This allows short reaction times with the least possible damage to the molecule. The starting compounds for the tritiation were ]ACTH( 1-24). Both tritiations were quantitative and yielded products of high purity, full biological activity, and with a specific radioactivity of 115 Ci/mrnol and 100 Ci/mmol, respectively.

Introduction. -The study of receptors for a -melanotropin (a-MSH) and adrenocorticotropin (ACTH) on adrenal cells, pigment cells, and in the brain requires biologically active hormones of high specific radioactivity. '251-Labelling has proved useful for CI -') Parts of this report have been presented at the 9th American Peptide Symposium, Toronto, June, 1985.

Nomenclature and abbreviations, see [I]. Additional abbreviations: HMPTA = hexamethylphosphoric triamide; ACTH = adrenocorticotropin; MSH = rnelanotropin (rnelanocyte-stimulating hormone); Msoc = 2-(methylsulfony1)ethoxycarbonyl; Pap = 4-azidophenylalanine; Pra = propargylglycine. All chiral amino acids are in the L-configuration.