Premium
Radiosynthesis of new radio neurotensin (8‐13) analogues
Author(s) -
Terriere D.,
Chavatte K.,
Ceusters M.,
Tourwé D.,
Mertens J.
Publication year - 1998
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/(sici)1099-1344(199801)41:1<19::aid-jlcr48>3.0.co;2-t
Subject(s) - chemistry , neurotensin , radiosynthesis , labelling , yield (engineering) , peptide , stereochemistry , chelation , specific activity , nucleophile , radiochemistry , chromatography , neuropeptide , organic chemistry , biochemistry , receptor , in vivo , enzyme , materials science , microbiology and biotechnology , metallurgy , biology , catalysis
Abstract Two types of radiolabelled neurotensin(8‐13) analogues have been synthesised. For radioiodination 2‐ and 4‐bromophenyl‐acetyl and 2‐ and 4‐bromobenzoyl Arg 8 substituted neurotensin(8‐13) were used as substrates for radiolabelling carried out by the Cu 1+ assisted non‐isotopic nucleophilic exchange with a labelling yield ranging from 55 to 85% depending on the position of the bromo atom in the phenyl ring. For labelling with 111 In, DTPA was substituted as chelating group on the Arg 8 position of neurotensin(8‐13). Labelling was achieved in kit‐conditions with a yield of 98%. The non carrier added peptide analogue was recovered by HPLC with a purity >99% and a specific activity of at least 370 TBq/mmol. The inhibition constant values for the binding of [ 3 H]neurotensin to guinea pig fore brain membranes were of the order of 7.5 nM for the halophenyl compounds and 6.5 nM for the DTPA substituted analogue. © 1998 John Wiley & Sons, Ltd.