Peptide labeling using 188Re, 188Re-MAG3 and 153Sm-H1ETA: A comparison on their in vitro lipophilicity |
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| Authors: | G Ferro-Flores F De M Ramírez MG Martínez-mendoza C Arteaga de Murphy M Pedraza-lópez L García-salinas |
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| Affiliation: | (1) Departamento de Materiales Radiactivos, Instituto Nacional de Investigaciones Nucleares, Estado de México, México;(2) Departamento de Química, Instituto Nacional de Investigaciones Nucleares, Estado de México, México;(3) Departamento de Medicina Nuclear, Instituto Nacional de Ciencias Médicas y Nutrición Salvador Zubirán, México D.F., México |
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| Abstract: | Lanreotide peptide was labeled with 153Sm-H1ETA and 188Re-MAG3 in order to evaluate whether or not their conjugation to the peptide produce significant differences of the in vitro lipophilicity with respect to the 188Re-lanreotide prepared by the direct labeling method (highly lipophilic). The differences of lipophilicity between the complexes, were evaluated using a reverse phase HPLC system. The measured lipophilicity of 153Sm-H1ETA-lanreotide, 188Re-MAG3-lanreotide and 188Re-lanreotide was taken to be the capacity factor k" = (t
R-t
0)/t
0 where t
R is the retention time and t
0 is the dead time] for each of the complexes under identical chromatography conditions. Results showed that the in vitro lipophilicity decreased in the order 188Re-lanreotide (direct labeling), 188Re-MAG3-lanreotide and 153Sm-H1ETA-lanreotide. Since the last one has a capacity factor (k") similar to that of 188Re-MAG3, some renal elimination for 153Sm-H1ETA-lanreotide could be expected, which probably would reduce the unnecessary radiation dose to normal tissues. |
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