PT  - JOURNAL ARTICLE
AU  - Kuo-Hsing Ma
AU  - Wen-Sheng Huang
AU  - Chi-Jiun Peng
AU  - Jeng-Jong Hwang
AU  - Ren-Shyan Liu
AU  - Chyng Yann Shiue
TI  - In vivo measurement of paroxetine binding on serotonin transporters using 4-[18F]-ADAM micro-PET in rats
DP  - 2007 May 01
TA  - Journal of Nuclear Medicine
PG  - 245P--245P
VI  - 48
IP  - supplement 2
4099  - http://jnm.snmjournals.org/content/48/supplement_2/245P.2.short
4100  - http://jnm.snmjournals.org/content/48/supplement_2/245P.2.full
SO  - J Nucl Med2007 May 01; 48
AB  - 1138 Objectives: N, N-Dimethyl-2-(2-amino-4-[18F]-fluorophenylthio) benzylamine (4-18F-ADAM) is a novel radiotracer for in vivo imaging of serotonin transporter (SERT). In this study, we evaluated the biodistribution and specificity of 4-18F-ADAM in control and paroxetine-treated rat brains using micro-PET and autoradiography, respectively. Methods: The brain biodistribution of 4-18F-ADAM was accessed via micro-PET and autoradiography by injecting intraveneously the radiotracer into the rats. Additionally, rats were pre-treated with different doses of paroxetine (ranged from 0.01 to 0.5 mg/kg) at 10-15 minutes before 4-18F-ADAM injection to evaluate the specificity of the radiotracer. The specific uptake ratios (SUR) of 4-[18F]-ADAM were calculated by drawing the regions of interest (ROI) in various areas of rat brains in reference to the cerebellum (i.e., [ROI-cerebellum]/cerebellum). Results: We found that the distribution of 4-[18F]-ADAM binding was consistent with the known distribution of SERT regions in the rat brain. Both the micro-PET and autoradiographic studies showed that the highest uptake of 4-[18F]-ADAM is located at raphe nucleus, high to modest uptake at superior colliculus, substantia nigra, hypothalamus, thalamus, and neocortex, and lowest uptake at cerebellum. In normal control rats, the 4-[18F]-ADAM SUR values ranged from about 2.1 in the neocortex to 4.7 in the raphe nucleus in the micro-PET studies, which are comparable with the results from the autoradiographic studies. After i.v. injected paroxetine into the rats, the 4-[18F]-ADAM uptake was significantly reduced in almost all the brain regions. Both the micro-PET and autoradiographic studies showed the decreases of 4-[18F]-ADAM uptake were in a dose-dependent pattern after paroxetine treatment. Conclusions: Our results suggest that the 4-[18F]-ADAM may be a useful radiotracer for monitoring in vivo changes in SERT of rat brains.