Carbon-11 labeled radioligands for imaging brain cannabinoid receptors.
Two radioligands, [(11)C] SR149080 and its morpholino analog [(11)C] SR149568, were synthesized by reaction of the respective phenolic precursors with [(11)C] methyl iodide. Both radioligands had appropriate regional brain distribution for cannabinoid receptors in mice with peak target to non-target ratios of 2.2 for [(11)C] SR149080 and 1.6 for [(11)C] SR149568 at 90 and 30 minutes post-injection respectively. The uptake of both tracers was blocked with a 1 mg/kg dose of SR141716A.
Mathews
William B
WB
Department of Radiology, Johns Hopkins University, Baltimore, MD 21287, USA. bmathews@petscan.nm.jhu.edu
Scheffel
Ursula
U
Rauseo
Paige A
PA
Ravert
Hayden T
HT
Frank
Richard A
RA
Ellames
George J
GJ
Herbert
John M
JM
Barth
Francis
F
Rinaldi-Carmona
Murielle
M
Dannals
Robert F
RF
D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism*; D002250:Carbon Radioisotopes / Q000493:pharmacokinetics*; D008297:Male; D051379:Mice; D009025:Morpholines / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D010880:Piperidines / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D011720:Pyrazoles / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics; D043882:Receptors, Cannabinoid; D011955:Receptors, Drug / Q000378:metabolism*; D012680:Sensitivity and Specificity
D002250:Carbon Radioisotopes; D009025:Morpholines; C471423:N-(piperidin-1-yl)-5-(4-methoxyphenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide; D010880:Piperidines; D011720:Pyrazoles; D019275:Radiopharmaceuticals; D043882:Receptors, Cannabinoid; D011955:Receptors, Drug; C471424:SR 149568