A distribution study of 11C platelet-activating factor (PAF) analogs in normal and tumor-bearing mice.

Abstract

As a preliminary study to image platelet-activating factor (PAF) receptors in vivo, comparative study of biodistribution between 1-O-hexadecy1-2-O-N, N-dimethylcarbamoyl-sn-glycero-3-phosphocholine [choline-methyl-11C](L-[11C]dimethylcarbamoyl-PAF) and nonspecific PAF analog, 3-O-hexadecyl-2-O-N,N-dimethylcarbamoyl-sn-glycero-1-phosphocholine [choline-methyl-11C](D-[11C]-dimethylcarbamoyl-PAF) was carried out in both normal and tumor-bearing mice. Higher accumulation of L-[11C]dimethylcarbamoyl-PAF than D-[11C]dimethylcarbamoyl-PAF was observed in normal mice spleen. The co-administration of PAF antagonists dose-dependently reduced the radioactivity level of the L-isomer only in the spleen. In mice bearing Ehrlich tumors and Sarcoma 180, more L-than the D-[11C]-isomer was accumulated in the tumor and spleen. We found that specific accumulation sites for L-[11C]dimethylcarbamoyl-PAF exist in the spleen and tumors than in other tissues. Moreover, the comparison of accumulation between L- and D-[11C] dimethylcarbamoyl-PAF would be a useful procedure for estimation of PAF receptors in vivo.

• Authors: T Sasaki, T Tohyama, K Oda, H Toyama, S Ishii, M Senda, K Karasawa, N Satoh, M Setaka, S Nojima, T Nozaki, P Braquet
• Journal: Nuclear medicine and biology (Nucl Med Biol) Vol. 23 Issue 3 Pg. 309-14 (Apr 1996) ISSN: 0969-8051 [Print] United States
• PMID: 8782242 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• 1-O-hexadecyl-2-O-N,N-dimethylcarbamoyl-sn-glycero-3-phosphocholine
• Carbon Radioisotopes
• Platelet Activating Factor
• Platelet Membrane Glycoproteins
• Receptors, Cell Surface
• Receptors, G-Protein-Coupled
• platelet activating factor receptor

Topics

• Animals
• Carbon Radioisotopes
• Kinetics
• Male
• Mice
• Mice, Inbred Strains
• Platelet Activating Factor (analogs & derivatives, chemical synthesis, pharmacokinetics)
• Platelet Membrane Glycoproteins (analysis, metabolism)
• Receptors, Cell Surface
• Receptors, G-Protein-Coupled
• Reference Values
• Sarcoma 180 (metabolism)
• Stereoisomerism
• Tissue Distribution