1121932-61-3Relevant academic research and scientific papers
New positron emission tomography (PET) radioligand for imaging σ-1 receptors in living subjects
James, Michelle L.,Shen, Bin,Zavaleta, Cristina L.,Nielsen, Carsten H.,Mesangeau, Christophe,Vuppala, Pradeep K.,Chan, Carmel,Avery, Bonnie A.,Fishback, James A.,Matsumoto, Rae R.,Gambhir, Sanjiv S.,McCurdy, Christopher R.,Chin, Frederick T.
, p. 8272 - 8282 (2012)
σ-1 receptor (S1R) radioligands have the potential to detect and monitor various neurological diseases. Herein we report the synthesis, radiofluorination, and evaluation of a new S1R ligand 6-(3-fluoropropyl)-3-(2- (azepan-1-yl)ethyl)benzo[d]thiazol-2(3H)-one ([18F]FTC-146, [ 18F]13). [18F]13 was synthesized by nucleophilic fluorination, affording a product with >99% radiochemical purity (RCP) and specific activity (SA) of 2.6 ± 1.2 Ci/μmol (n = 13) at end of synthesis (EOS). Positron emission tomography (PET) and ex vivo autoradiography studies of [18F]13 in mice showed high uptake of the radioligand in S1R rich regions of the brain. Pretreatment with 1 mg/kg haloperidol (2), nonradioactive 13, or BD1047 (18) reduced the binding of [18F]13 in the brain at 60 min by 80%, 82%, and 81%, respectively, suggesting that [ 18F]13 accumulation in mouse brain represents specific binding to S1Rs. These results indicate that [18F]13 is a promising candidate radiotracer for further evaluation as a tool for studying S1Rs in living subjects.
