Labelling and evaluation of new stabilised neurotensin (8-13) analogues for single photon emission tomography (SPET)

Autor:	D. Terriere, Kris Chavatte, L. Jeannin, Axel Bossuyt, E. Bruyneel, Dirk Tourwé, Jan A.J. Schuurkes, M.R. Briejer, K. Iterbeke, J. Mertens, J. E. Leysen
Rok vydání:	1999
Předmět:	chemistry.chemical_classification Biodistribution Tetrapeptide Organic Chemistry Peptide Biochemistry Analytical Chemistry Amino acid chemistry.chemical_compound chemistry In vivo Drug Discovery Peptide synthesis Radiology Nuclear Medicine and imaging Neurotensin receptor Spectroscopy Neurotensin
Zdroj:	Journal of Labelled Compounds and Radiopharmaceuticals. 42:423-435
ISSN:	1099-1344 0362-4803
DOI:	10.1002/(sici)1099-1344(199905)42:5<423::aid-jlcr201>3.0.co;2-s
Popis:	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 live 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.
Databáze:	OpenAIRE
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