Radiosynthesis of sigma receptor ligands for positron emission tomography: 11C- and 18F-labeled guanidines.
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.
Wilson
A A
AA
Division of Nuclear Medicine, Johns Hopkins Medical Institutions, Baltimore, Maryland 21205-2179.
Dannals
R F
RF
Ravert
H T
HT
Sonders
M S
MS
Weber
E
E
Wagner
H N
HN
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
D002250:Carbon Radioisotopes; D005462:Fluorine Radioisotopes; D006146:Guanidines; D011957:Receptors, Opioid; D017480:Receptors, sigma; C050232:1,3-ditolylguanidine