title: Sigma receptors are expressed in human non-small cell lung carcinoma.
abstract: N-(2-piperidinoethyl)4-iodobenzamide), IPAB, was used to characterize sigma receptors in non-small cell lung cancer (NSCLC) cell lines. 125IPAB bound with high affinity to large cell carcinoma (NCI-H1299), adenocarcinoma (NCI-H838), and lung carcinoid (NCI-H727) cell lines. Specific IPAB binding was inhibited with high affinity by haloperidol (Ki = 0.6 nM), IPAB (Ki = 14 nM) and 1,3-ditolyl guanidine (DTG) (Ki = 40 nM). Relative to other receptor ligands, IPAB was not readily internalized at 37 degrees C. IPAB had little effect on the growth of NSCLC cells. Scintigraphic imaging studies using 131IPAB in nude mice bearing NCI-H838 xenografts visualized the tumor at 24 or 30 hours after injection. These results suggest that sigma receptors which are present on NSCLC cells may be used as external markers for imaging tumors in vivo.
authors.affiliation: Department of Radiology, George Washington University Medical Center, Washington, DC 20037, USA.
authors.forename: C S
authors.initials: CS
authors.lastname: John
authors.forename: W D
authors.initials: WD
authors.lastname: Bowen
authors.forename: V M
authors.initials: VM
authors.lastname: Varma
authors.forename: J G
authors.initials: JG
authors.lastname: McAfee
authors.forename: T W
authors.initials: TW
authors.lastname: Moody
mesh_terms: D000818:Animals; D002289:Carcinoma, Non-Small-Cell Lung / Q000378:metabolism*; D005260:Female; D006801:Humans; D007457:Iodine Radioisotopes; D008175:Lung Neoplasms / Q000378:metabolism*; D051379:Mice; D008819:Mice, Nude; D011869:Radioligand Assay; D017480:Receptors, sigma / Q000096:biosynthesis*; D014407:Tumor Cells, Cultured
chemical_list: D007457:Iodine Radioisotopes; D017480:Receptors, sigma