Automatic synthesis of ¹⁸F-AV-45 and its clinical application in Alzheimer's disease

To investigate the automatic synthesis of β-amyloid (Aβ) positron emission tomography (PET) imaging agent (E) -4- (2- (6- (2- (2-¹⁸F fluoroethoxy) ethoxy) ethoxy) pyridine-3-yl) vinyl) - N-methylaniline (¹⁸F-AV-45) for the diagnosis of Alzheimer's disease (AD) and its clinical application in AD patients.

Fluorine-18-AV-45 was synthesized with AV-105 as the precursor, and the factors affecting the synthesis efficiency, such as the amount of precursor, nucleophilic reaction temperature were studied. At the same time, ¹⁸F-AV-45 PET/computed tomography (CT) brain scanning was performed in 15 patients with dementia to determine whether AD was the cause of the dementia.

After optimizing the parameters, it was discovered that the highest synthesis efficiency was achieved with a AV-105 dosage of 2mg, a reaction temperature of 130^oC, and 1mL of DMSO. The radiochemical yield (RCP) was greater than 98, and the uncorrected synthesis efficiency was about 31.0%±2.8%. Ten of the 15 patients with dementia showed positive Aβ protein deposition, and the main deposition site of the imaging agent was the gray matter area of the brain, which was consistent with AD diagnosis, while the other 5 patients showed negative Aβ protein deposition, suggesting non-AD dementia.

β-amyloid protein ¹⁸F-AV-45 imaging agent can be easily and quickly prepared by the All in One radiochemical synthesis module. Our preliminary results offer hope that it can effectively detect β-amyloid deposition in the brain of AD patients in order to determine the etiology of dementia.