449729-47-9Relevant academic research and scientific papers
Radiosynthesis and evaluation of [11C-carbonyl ]-labeled carbamates as fatty acid amide hydrolase radiotracers for positron emission tomography
Wilson, Alan A.,Hicks, Justin W.,Sadovski, Oleg,Parkes, Jun,Tong, Junchao,Houle, Sylvain,Fowler, Christopher J.,Vasdev, Neil
, p. 201 - 209 (2013/03/14)
Fatty acid amide hydrolase (FAAH) plays a key role in regulating the tone of the endocannabinoid system. Radiotracers are required to image and quantify FAAH activity in vivo. We have synthesized a series of potent FAAH inhibitors encompassing two classes of N-alkyl-O-arylcarbamates and radiolabeled eight of them with carbon-11. The [11C-carbonyl]-radiotracers were evaluated in vitro and ex vivo in rats as potential FAAH imaging agents for positron emission tomography (PET). Both sets of [11C]O-arylcarbamates showed good to excellent brain penetration and an appropriate regional distribution. Pretreatments with a FAAH inhibitor demonstrated that 80-95% of brain uptake of radioactivity constituted binding of the radiotracers to FAAH. Brain extraction measurements showed that binding to FAAH was irreversible and kinetically different for the two classes of carbamates. These promising results are discussed in terms of the requirements of a suitable radiotracer for the in vivo imaging of FAAH using PET.
Synthesis and application of isocyanates radiolabeled with carbon-11
Wilson, Alan A.,Garcia, Armando,Houle, Sylvain,Sadovski, Oleg,Vasdev, Neil
scheme or table, p. 259 - 264 (2011/03/19)
Carbon-11 labeled isocyanates are efficiently prepared by dehydration of [11C]carbamate salts, which in turn are easily formed from cyclotron-produced [11C]CO2 and amines in the presence of a CO2 fixation agent. The [11C]isocyanates are useful radiosynthons for the synthesis of a variety of [carbonyl-11C]- labeled asymmetrical ureas and carbamate esters. The method is well suited to incorporate any isotope of carbon, and is especially useful for positron emission tomography (PET) radiotracers for in vivo imaging. This is demonstrated by using the method to make [carbonyl-11C]-6-hydroxy-[1,1′- biphenyl]-3-yl cyclohexylcarbamate which is a novel radiotracer for PET imaging of fatty acid amide hydrolase.
