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• W1966853844 abstract "Neurotensin(8–13) (NTS(8–13)) analogs with C- and/or N-terminal β-amino acid residues and three DOTA derivatives thereof have been synthesized (i.e., 1–6). A virtual docking experiment showed almost perfect fit of one of the 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) derivatives, 6a, into a crystallographically identified receptor NTSR1 (Fig. 1). The affinities for the receptors of the NTS analogs and derivatives are low, when determined with cell-membrane homogenates, while, with NTSR1-exhibiting cancer tissues, affinities in the single-digit nanomolar range can be observed (Table 2). Most of the β-amino acid-containing NTS(8–13) analogs (Table 1 and Fig. 2), including the 68Ga complexes of the DOTA-substituted ones (6; Figs. 2 and 5), are stable for ca. 1 h in human serum and plasma, and in murine plasma. The biodistributions of two 68Ga complexes (of 6a and 6b) in HT29 tumor-bearing nude mice, in the absence and in the presence of a blocking compound, after 10, 30, and 60 min (Figs. 3 and 4) lead to the conclusion that the amount of specifically bound radioligand is rather low. This was confirmed by PET-imaging experiments with the tumor-bearing mice (Fig. 6). Comparison of the in vitro plasma stability (after 1 h) with the ex vivo blood content (after 10–15 min) of the two 68Ga complexes shows that they are rapidly cleaved in the animals (Fig. 5)." @default.
• W1966853844 created "2016-06-24" @default.
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• W1966853844 date "2013-12-01" @default.
• W1966853844 modified "2023-10-17" @default.
• W1966853844 title "Syntheses, Receptor Bindings,<i>in vitro</i>and<i>in vivo</i>Stabilities and Biodistributions of DOTA-Neurotensin(8-13) Derivatives Containing<i>β</i>-Amino Acid Residues - A Lesson about the Importance of Animal Experiments" @default.
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• W1966853844 doi "https://doi.org/10.1002/cbdv.201300331" @default.
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