title: Radiosynthesis of sigma receptor ligands for positron emission tomography: 11C- and 18F-labeled guanidines.
abstract: A series of analogues of the potent and selective sigma receptor ligand 1,3-ditolylguanidine (DTG) were synthesized and demonstrated to have high affinity for the sigma receptor as measured by in vitro [3H]DTG displacement studies using guinea pig brain tissue. Three of these 1-aryl-3-(1-adamantyl)guanidines were radiolabeled--two with carbon-11 and one with fluorine-18. Radiochemical yields and specific activities were sufficient for these radiotracers to be used in positron emission tomography imaging of the haloperidol-sensitive sigma receptor.
authors.affiliation: Division of Nuclear Medicine, Johns Hopkins Medical Institutions, Baltimore, Maryland 21205-2179.
authors.forename: A A
authors.initials: AA
authors.lastname: Wilson
authors.forename: R F
authors.initials: RF
authors.lastname: Dannals
authors.forename: H T
authors.initials: HT
authors.lastname: Ravert
authors.forename: M S
authors.initials: MS
authors.lastname: Sonders
authors.forename: E
authors.initials: E
authors.lastname: Weber
authors.forename: H N
authors.initials: HN
authors.lastname: Wagner
mesh_terms: D000818:Animals; D002250:Carbon Radioisotopes; D002851:Chromatography, High Pressure Liquid; D005462:Fluorine Radioisotopes; D006146:Guanidines / Q000138:chemical synthesis* / Q000378:metabolism; D006168:Guinea Pigs; D009682:Magnetic Resonance Spectroscopy; D011957:Receptors, Opioid / Q000378:metabolism*; D017480:Receptors, sigma; D014055:Tomography, Emission-Computed
chemical_list: D002250:Carbon Radioisotopes; D005462:Fluorine Radioisotopes; D006146:Guanidines; D011957:Receptors, Opioid; D017480:Receptors, sigma; C050232:1,3-ditolylguanidine