Radioiodinated diacylglycerol analogues and methods of use

Details Radioiodinated diacylglycerol analogues and methods of use Radioiodinated diacylglycerol analogues and methods of use

1987-06-12

1990-05-15

Maples, John S.

Drug, bio-affecting and body treating compositions

Radionuclide or intended radionuclide containing; adjuvant...

424 9, 260408, A61K 4902, A61K 4900

Patent

active

049256491

ABSTRACT:
Novel iodinated and radioiodinated 1,2-diacylglycerol analogues are biological reagents for studying the effect of diacylglycerols in the activation of protein kinase C. This calcium-requiring enzyme may be involved in tumor promotion by phorbol diesters and related compounds. Iodinated and radioiodinated 1,2-diacylglycerol analogues, in accordance with the invention, are useful as imaging agents, such as radiopaques and radiopharmaceuticals, and have the general formula: ##STR1## The triglycerol backbone structure is 1,2-disubstituted with one position being occupied by an iodine-containing substituent, preferably an amino-substituted-2,4,6-triiodophenyl aliphatic chain, such as iopanoic acid, or by a monoiodiphenyl aliphatic chain, such as (m-iodophenyl)propanoic acid. The other position may be substituted with saturated and unsaturated long and short aliphatic chains.

REFERENCES:
Weichert, J. et al. "Lipid Soluble Contrast Agents for Hepatic CT Imaging", Acs Meeting Abstract No. 29, Washington, DC 8/1983.

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