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Development of an In Vivo Method to Estimate Effective Drug Doses and Quantify Fatty Acid Amide Hydrolase in Rodent Brain using Positron Emission Tomography Tracer [C-11]DFMC
Fatty acid amide hydrolase (FAAH) is a key enzyme in the endocannabinoid system. N-(3,4-Dimethylisoxazol-5-yl)piperazine-4-(4-(2-fluoro-4-[C-11]methylphenyl)thiazol-2-yl]-1-carboxamide ([C-11]DFMC) was developed as an irreversible-type positron emission tomography (PET) tracer for FAAH. Here, we attempted to non invasively estimate rate constant k(3) (rate of transfer to the specifically-bound compartment) as a direct index for FAAH in the rat brain. First, the two-tissue compartment model analysis including three parameters [K-1-k(3), two-tissue compartment model for the irreversible-type radiotracer (2TCMi)] in PET study with [C-11] DFMC was conducted, which provided 0.21 +/- 0.04 ml.cm(-3).min(-1 )of the net uptake value (K-i), an indirect index for FAAH, in the FAAH-richest region (the cingulate cortex). Subsequently, to noninvasively estimate K-i value, the reference model analysis (Patlak graphical analysis reference model) was tried using a time-activity curve of the spinal cord. In that result, the noninvasive K-i value (K-REF) was concisely estimated with high correlation (r > 0.95) to K-i values based on 2TCMi. Using estimated K-REF value, we tried to obtain calculated-k(3) based on previously defined equations. The calculated k(3) was successfully estimated with high correlation (r= 0.95) to direct k(3) in 2TCMi. Finally, the dose relationship study using calculated k(3) demonstrated that in vivo ED50 value of [3-(3-carbamoylphenyl)phenyl] N-cyclohexylcarbamate, a major inhibitor of FAAH, was 66.4 mu g/kg in rat brain. In conclusion, we proposed the calculated k(3) as an alternative index corresponding to regional FAAH concentrations and suggested that PET with [C-11]DFMC enables occupancy study for new pharmaceuticals targeting FAAH. SIGNIFICANCE STATEMENT In the present study, we proposed calculated k(3) as an alternative index corresponding with fatty acid amide hydrolase concentration. By using calculated k(3), in vivo ED(50 )of [3-(3-carbamoylphenyl)phenyl] N-cyclohexylcarbamate was successfully estimated to be 66.4 mu g/kg for rats. Thus, we demonstrated the pharmacological utility of positron emission tomography with N-(3,4-dimethylisoxazol-5-yl)piperazine-4-[4-(2-fluoro-4-[C-11]nnethylphenyl)thiazol-2 -yl]-1-carboxamide.
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Reference:
Piperazine – Wikipedia,
,Piperazines – an overview | ScienceDirect Topics