Premium
Labelling and evaluation of new stabilised neurotensin (8–13) analogues for single photon emission tomography (SPET)
Author(s) -
Chavatte K.,
Terriere D.,
Jeannin L.,
Iterbeke K.,
Briejer M.,
Schuurkes J.,
Mertens J. J. R.,
Bruyneel E.,
Tourwé D.,
Leysen J. E.,
Bossuyt A.
Publication year - 1999
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(199905)42:5<423::aid-jlcr201>3.0.co;2-s
Subject(s) - neurotensin , chemistry , isostere , biodistribution , labelling , neurotensin receptor , receptor , oligopeptide , peptide , chemical synthesis , radiochemistry , stereochemistry , pharmacology , neuropeptide , biochemistry , in vitro , medicine
Neurotensin(8–13) analogues were biologically stabilised by replacement of the peptide bond between amino acids 8 and 9 by the reduced ψ(CH 2 ‐NH) isostere. Diethylenetriaminepentaacetic acid (DTPA) analogues for In‐111 labelling and 2‐bromo‐phenyl‐acetyl analogues for radioiodination, showed receptor affinities in the nanomolar range in combination with a biological half life in human plasma up to 275 minutes. Biodistribution studies in male Wistar rats of metabolically stabilised and non‐stabilised 111 In‐DTPA‐NT(8–13) analogues showed a major clearance from the blood through the kidneys. 125 I‐Labelled neurotensin (8–13) analogues showed accumulation up to 2.2% of the injected dose per g tissue in the liver which might be an important disadvantage when diagnosis of tumours in the gut is aimed. Neurotensin(8–13) analogues labelled with In‐111 or I‐123 may act as new potential peptidergic radiopharmaceuticals for SPET diagnosis of neurotensin receptor (NTR) positive tumours. Copyright © 1999 John Wiley & Sons, Ltd.