502487-28-7Relevant academic research and scientific papers
Synthesis, structure-activity relationship, and evaluation of SR141716 analogues: Development of central cannabinoid receptor ligands with lower lipophilicity
Katoch-Rouse, Reeti,Pavlova, Olga A.,Caulder, Tara,Hoffman, Alexander F.,Mukhin, Alexey G.,Horti, Andrew G.
, p. 642 - 645 (2007/10/03)
Exploration of the central CB1 cannabinoid receptors using positron emission tomography (PET) will allow for an understanding of the pharmacological and physiological role played by these receptors in the CNS. Current tracers are highly lipophi
Synthesis of N-(piperidin-1-yl)-5-(4-methoxyphenyl)-1-(2-chlorophenyl)-4- [18F]fluoro-1H-pyrazole-3-carboxamide by nucleophilic [18F] fluorination: A PET radiotracer for studying CB1 cannabinoid receptors
Katoch-Rouse, Reeti,Horti, Andrew G.
, p. 93 - 98 (2007/10/03)
The feasibility of nucleophilic displacement of bromide in the 4-bromopyrazole ring with [18F]fluoride has been demonstrated by the synthesis of two radiolabeled compounds: N-(piperidin-1-yl)-5-(4-methoxyphenyl)-1- (2-chlorophenyl)-4-[18F]fluoro-1H -pyrazole-3-carboxamide, ([18F] NIDA-42033) 1b and 1-(2-chlorophenyl)-4-[18F]fluoro-5-(4-methoxyphenyl)- 1H-pyrazole-3-carboxylic acid, ethyl ester 4. The radiochemical yields were in the range of 1-6%. [18]NIDA-42033, a potential radiotracer for the study of CB1 cannabinoid receptors in the animal brain by positron emission tomography, has been synthesized in sufficient quantities with specific radioactivity greater than 2500 mCi/μmol and radiochemical purity >95%. Copyright
