125I-iodinated benzazepines bind to melanin: implications for the noninvasive localization of pigmented melanomas.
|
| Abstract |
Both the 5-R and the 5-S enantiomers of [125I]2,3,4,5-tetrahydro-8-iodo-3-methyl-5-phenyl-1H-3-benzazepin- 7-ol bind to melanin. The interaction between the 5-R enantiomer and melanin permits visualization of melanomas in mice with a noninvasive imaging procedure. Two lines of evidence suggest that the interaction between iodinated ligands and melanin is not related to the D-1 dopamine receptor, a known target for the 5-R enantiomer: first, melanin binds both enantiomers of the 125I-iodinated benzazepine while the D-1 receptor binds only the 5-R enantiomer; second, the melanin binding site displays only a 5-fold difference in affinity towards the R- and S-enantiomers of SCH 23390 while the D-1 receptor displays a 100-fold difference in affinity towards these two molecules. Because both enantiomers of the iodinated benzazepine bind to a human pigmented melanoma, we propose that such compounds may be of use in the diagnosis of pigmented melanoma: in addition, we discuss the possible application of these molecules as a supplement to existing technology for the localization of pigmented melanomas.
|
|---|---|
| Authors | T Agui, G Bryant, J W Kebabian, S Larson, J M Saavedra, K Shigematsu, T Yamamoto, K Yokoyama |
| Journal | International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology (Int J Rad Appl Instrum B) Vol. 14 Issue 2 Pg. 133-41 ( 1987) ISSN: 0883-2897 [Print] England |
| PMID | 2885295 (Publication Type: Journal Article) |
| Chemical References |
|
| Topics |
|
Join CureHunter, for free Research Interface BASIC access!
Realize the full power of the drug-disease research graph!