Abstract | UNLABELLED: The development of an effective radiopharmaceutical with affinity for malignant melanoma has been a research goal for some time. The early detection of melanoma metastases would greatly improve the therapy outcome for this disease. This article describes the synthesis of radioiodinated IMBA, N-(2-diethylaminoethyl)-3-[123I/131I]iodo-4-methoxybenzamide 8, its organ distribution, its comparison with BZA and other benzamides, and demonstrates the scintigraphic efficacy of the title compound with three melanoma patients. METHODS: RESULTS: While structural changes in the amide substituents of N-(2-dialkylaminoalkyl)-4-iodobenzamides 2-7 resulted in no improvement in organ distribution compared with BZA, the 3-iodo-4-methoxyphenyl form of IMBA showed high melanoma uptake with significantly higher melanoma/nontarget tissue ratios. Compared with BZA the average ratio improved after 1 hr by a factor of eight and was still four times better after 6 hr. BZA and IMBA exhibit almost identical n-octanol/ phosphate buffer partition coefficients, however, IMBA has a faster urinary excretion facilitated by a lower affinity to erythrocytes and serum proteins; this could explain the improved tissue partinioning observed. Scintigraphy of patients with melanoma metastases confirmed the promising characteristics derived from the animal studies. CONCLUSION:
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Authors | C Nicholl, A Mohammed, W E Hull, B Bubeck, M Eisenhut |
Journal | Journal of nuclear medicine : official publication, Society of Nuclear Medicine
(J Nucl Med)
Vol. 38
Issue 1
Pg. 127-33
(Jan 1997)
ISSN: 0161-5505 [Print] United States |
PMID | 8998166
(Publication Type: Case Reports, Journal Article)
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Chemical References |
- Benzamides
- Contrast Media
- Iodine Radioisotopes
- Radiopharmaceuticals
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Topics |
- Animals
- Benzamides
(pharmacokinetics)
- Contrast Media
- Female
- Humans
- Iodine Radioisotopes
(pharmacokinetics)
- Isotope Labeling
(methods)
- Male
- Melanoma
(diagnostic imaging, metabolism, secondary)
- Melanoma, Experimental
(diagnostic imaging, metabolism)
- Mice
- Mice, Inbred C57BL
- Middle Aged
- Radionuclide Imaging
- Radiopharmaceuticals
(pharmacokinetics)
- Tissue Distribution
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