In vitro studies on the cellular uptake of melanoma imaging aminoalkyl-iodobenzamide derivatives (ABA).
The cellular uptake of 11 radioiodinated aminoalkyl-iodobenzamides (ABA) was studied using cultivated murine melanoma cells (B16/C3). All derivatives showed a high uptake (up to about 80%) of radioactivity in melanotic melanoma cells; hence, accumulation of all compounds radioiodinated in the ortho position was reduced by approximately 30%. Using the compound para-[131I]iododiethyl-aminoethylbenzamide (p-131I-ABA-2-2) a close correlation of the cellular melanin content with the tracer uptake (R2 = 0.95) was verified. The presence of extracellular melanin, however, had no effect on the cellular tracer uptake. Because the accumulation was independent of the specific activity of p-131I-ABA-2-2, a significant contribution to the uptake process by binding to receptor sites could be excluded.
Dittmann
H
H
Institut für Med. Strahlenbiologie, Universitätsklinikum Essen, Germany.
Coenen
H H
HH
Zölzer
F
F
Dutschka
K
K
Brandau
W
W
Streffer
C
C
D001549:Benzamides / Q000378:metabolism*; D007457:Iodine Radioisotopes; D007463:Iodobenzoates / Q000378:metabolism*; D008543:Melanins / Q000096:biosynthesis; D008545:Melanoma / Q000000981:diagnostic imaging* / Q000378:metabolism; D008954:Models, Biological; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000378:metabolism; D017480:Receptors, sigma / Q000378:metabolism; D012680:Sensitivity and Specificity; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D001549:Benzamides; D007457:Iodine Radioisotopes; D007463:Iodobenzoates; D008543:Melanins; D019275:Radiopharmaceuticals; D017480:Receptors, sigma; C066918:N-(2-(diethylamino)ethyl)-4-iodobenzamide