title: N-(n-Benzylpiperidin-4-yl)-2-[18F]fluorobenzamide: a potential ligand for PET imaging of breast cancer.
abstract: N-(N-Benzylpiperidin-4-yl)-2-[(18)F]fluorobenzamide (2), a potential ligand for PET imaging of sigma receptor, has been found to be a potential agent for detection of breast cancer. In vivo studies in severe combined immunodeficient (SCID) mice bearing MDA-MB231 tumors showed that the uptake of compound 2 in these tumors was high (3.8%/g); the ratios of tumor/muscle and tumor/blood were 6.2 and 7.0, respectively, at 1 h postinjection. Pretreatment of SCID mice with haldol increased the uptake of compound 2 in blood, muscle, and other well-perfused organs while decreasing its uptake in tumors. The ratios of tumor/muscle and tumor/blood decreased from 6.2 and 7.0 to 1.3 and 1.1, respectively, at 1 h postinjection. At 2 h postinjection, the ratios of tumor/muscle and tumor/blood decreased from 4.9 and 7.8 to 1.4 and 1.4, respectively. The tumor uptake of compound 2 in SCID mice bearing primary tumor explants from a human breast cancer patient was lower than that in MDA-MB231 tumors (1.66%/g versus 3.78%/g), and the ratios of tumor/muscle and tumor/blood were 3.5 and 3.7, respectively, at 1 h postinjection. These results suggest that compound 2 may be a potential ligand for PET imaging of breast cancer.
authors.affiliation: Department of Radiology, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA. shiue@rad.upenn.edu
authors.forename: C
authors.initials: C
authors.lastname: Shiue
authors.forename: G G
authors.initials: GG
authors.lastname: Shiue
authors.forename: F
authors.initials: F
authors.lastname: Benard
authors.forename: S
authors.initials: S
authors.lastname: Visonneau
authors.forename: D
authors.initials: D
authors.lastname: Santoli
authors.forename: A A
authors.initials: AA
authors.lastname: Alavi
mesh_terms: D000818:Animals; D001549:Benzamides / Q000378:metabolism* / Q000493:pharmacokinetics; D001943:Breast Neoplasms / Q000000981:diagnostic imaging*; D005260:Female; D006801:Humans; D051379:Mice; D016513:Mice, SCID; D009368:Neoplasm Transplantation; D010880:Piperidines / Q000378:metabolism* / Q000493:pharmacokinetics; D019275:Radiopharmaceuticals / Q000378:metabolism* / Q000493:pharmacokinetics; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed; D014407:Tumor Cells, Cultured
chemical_list: D001549:Benzamides; C109873:N-(N-benzylpiperidin-4-yl)-2-fluorobenzamide; D010880:Piperidines; D019275:Radiopharmaceuticals