| Uptake in melanoma cells of N-(2-diethylaminoethyl)-2-iodobenzamide (BZA2), an imaging agent for melanoma staging: relation to pigmentation. | |
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MedLine Citation:
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PMID: 15982575 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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N-(2-diethylaminoethyl)-2-iodobenzamide (BZA(2)) has been singled out as the most efficacious melanoma scintigraphy imaging agent. Our work was designed to assess the mechanisms of the specific affinity of the radioiodinated iodobenzamide for melanoma tissue. We studied the cellular uptake and retention of [(125)I]-BZA(2) on various cell lines. In vitro, cellular [(125)I]-BZA(2) uptake was related to the pigmentation status of the cells: higher in pigmented melanoma cell lines (M4 Beu, IPC 227, B 16) than in a nonpigmented one (M3 Dau) and nonmelanoma cell lines (MCF 7 and L 929). Two mechanisms were assessed: binding of the tracer to melanin or to sigma receptors of melanoma cells. First, the uptake of [(125)I]-BZA(2) after melanogenesis stimulation by alpha-melanocyte-stimulating hormone and l-tyrosine increased in the B 16 melanoma cell line both in vitro and in vivo according to melanin concentration. Moreover, the binding of [(125)I]-BZA(2) to synthetic melanin was dependent on melanin concentration and could be saturated. Second, no competition was evidenced on M4 Beu cells between [(125)I]-BZA(2) and haloperidol, a sigma ligand, at concentrations < or =10(-6) M. We show that the specificity and sensibility of BZA(2) as a melanoma scintigraphic imaging agent are mostly due to interactions with melanic pigments. |
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Authors:
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Sandrine Mansard; Janine Papon; Marie-France Moreau; Elisabeth Miot-Noirault; Pierre Labarre; Martine Bayle; Annie Veyre; Jean-Claude Madelmont; Nicole Moins |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Nuclear medicine and biology Volume: 32 ISSN: 0969-8051 ISO Abbreviation: Nucl. Med. Biol. Publication Date: 2005 Jul |
Date Detail:
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Created Date: 2005-06-28 Completed Date: 2005-12-07 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9304420 Medline TA: Nucl Med Biol Country: England |
Other Details:
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Languages: eng Pagination: 451-8 Citation Subset: IM |
Affiliation:
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Inserm, U484, Clermont-Ferrand, France. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Benzamides / pharmacokinetics* Cell Line, Tumor Haloperidol / metabolism Humans Male Melanins / metabolism Melanoma / metabolism*, pathology Mice Mice, Inbred C57BL Neoplasm Staging Pigmentation* Tissue Distribution |
| Chemical | |
Reg. No./Substance:
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0/Benzamides; 0/Melanins; 0/N-(2-(diethylamino)ethyl)-2-iodobenzamide; 52-86-8/Haloperidol |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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