In vitro studies on the cellular uptake of melanoma imaging aminoalkyl-iodobenzamide derivatives (ABA)

Nucl Med Biol. 1999 Jan;26(1):51-6. doi: 10.1016/s0969-8051(98)00046-8.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benzamides / metabolism*
  • Iodine Radioisotopes
  • Iodobenzoates / metabolism*
  • Melanins / biosynthesis
  • Melanoma / diagnostic imaging*
  • Melanoma / metabolism
  • Models, Biological
  • Radionuclide Imaging
  • Radiopharmaceuticals / metabolism
  • Receptors, sigma / metabolism
  • Sensitivity and Specificity
  • Structure-Activity Relationship
  • Tumor Cells, Cultured

Substances

  • Benzamides
  • Iodine Radioisotopes
  • Iodobenzoates
  • Melanins
  • Radiopharmaceuticals
  • Receptors, sigma
  • N-(2-(diethylamino)ethyl)-4-iodobenzamide