Premium
Synthesis of tritium labelled cholecystokinin derivative : [ 3 H]‐Boc‐[Nle 28, 31 ]‐ CCK 27–33
Author(s) -
Sasaki N. A.,
Funakoshi S.,
Potier P.,
Morgat J.L.,
Genet R.,
Gacel G.,
Charpentier B.,
Roques B. P.
Publication year - 1985
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580221104
Subject(s) - chemistry , norleucine , cholecystokinin , tritium , potency , stereochemistry , chemical synthesis , biological activity , derivative (finance) , specific activity , amino acid , biochemistry , in vitro , enzyme , receptor , leucine , physics , nuclear physics , financial economics , economics
The synthesis of a new acetylenic analogue of the C‐terminal heptapeptide segment of cholecystokinin (CCK) in which the Met 28 and Met 31 residues are replaced by two acetylenic precursors of norleucine (Nle), L‐2‐amino‐4‐hexynoic acid (Aha), is described. Reductive tritiation of this acetylenic heptapeptide Boc‐[Aha 28, 31 ]‐CCK 27, 33 led to the labelled [ 3 H]‐Boc‐[Nle 28, 31 ]‐CCK 27–33 which displays a specific activity of about 150 Ci/mmol. According to its full biological potency, this CCK analogue can be used for various biological assays including binding studies.