Tuyển tập báo cáo các nghiên cứu khoa học quốc tế ngành hóa học dành cho các bạn yêu hóa học tham khảo đề tài: Evaluation of 18F-nifene binding to a4b2 nicotinic receptors in the rat brain using microPET imaging | Kant et al. EJNMMI Research 2011 1 6 http content 1 1 6 9 EJNMMI Research a SpringerOpen Journal ORIGINAL RESEARCH Open Access Evaluation of 18F-nifene binding to a4p2 nicotinic receptors in the rat brain using microPET imaging Ritu Kant Cristian C Constantinescu Puja Parekh Suresh K Pandey Min-Liang Pan Balu Easwaramoorthy and Jogeshwar Mukherjee Abstract MicroPET imaging studies using 18F-nifene a new positron emission tomography PET radiotracer for nicotinic acetylcholinergic receptors nAChR a4p2 receptors in rats have been carried out. Rats were imaged for 90 min after intravenous injection of 18F-nifene to 1 mCi and binding potential BPND was measured. 18F-Nifene binding to thalamic and extrathalamic brain regions was consistent with the a4p2 nAChR distribution in the rat brain. Using the cerebellum as a reference the values for the thalamus varied less than 5 BPND n 3 confirming reproducibility of 18F-nifene binding. 18F-Nifene microPET imaging was also used to evaluate effects of nicotine in a group of Sprague-Dawley rats under isoflurane anesthesia. Nicotine challenge postadministration of 18F-nifene demonstrated reversibility of 18F-nifene binding in vivo. For a4p2 nAChR receptor occupancy nAChROCC various doses of nicotine 0 and mg kg nicotine free base 15 min prior to 18F-nifene were administered. Low-dose nicotine mg reached 80 nAChROCC while at higher doses mg 90 nAChROCC was measured. The small amount of 18F-nifene binding with reference to the cerebellum affects an accurate evaluation of nAChROCC. Efforts are underway to identify alternate reference regions for 18F-nifene microPET studies in rodents. Background Nicotinic a4p2 receptors play an important role in many CNS disorders such as Alzheimer s disease Parkinson s disease Schizophrenia mood disorders and nicotine dependence. Much work is being done on radiotracer compounds with high binding affinity as well as faster kinetics which can be .
