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Synthesis and Initial PET Imaging of New Potential NK1 Receptor Radioligands 1-[2-(3,5-bis-trifluoromethyl-benzyloxy)-1-phenyl-ethyl]-4-[11C]methyl-piperazine and {4-[2-(3,5-bis-trifluoromethyl-benzyloxy)-1-phenyl-ethyl]-piperazine-1-yl}-acetic Acid [11C]methyl Ester

Synthesis and Initial PET Imaging of New Potential NK1 Receptor Radioligands 1-[2-(3,5-bis-trifluoromethyl-benzyloxy)-1-phenyl-ethyl]-4-[11C]methyl-piperazine and {4-[2-(3,5-bis-trifluoromethyl-benzyloxy)-1-phenyl-ethyl]-piperazine-1-yl}-acetic Acid [11C]methyl Ester

Mingzhang Gao, Bruce H Mock, Gary D Hutchins, Qi-Huang Zheng

Nucl Med Biol. 2005 Jul;32(5):543-52.

PMID: 15982585

Abstract:

The NK(1) receptor radioligands 1-[2-(3,5-bis-trifluoromethyl-benzyloxy)-1-phenyl-ethyl]-4-[(11)C]methyl-piperazine ([(11)C]BMP, [(11)C]) and {4-[2-(3,5-bis-trifluoromethyl-benzyloxy)-1-phenyl-ethyl]-piperazine-1-yl}-acetic acid [(11)C]methyl ester ([(11)C]BME, [(11)C]) were synthesized for evaluation as new potential PET imaging agents for brain NK(1) receptors. The new tracers [(11)C]BMP and [(11)C]BME were prepared by N-[(11)C]methylation and O-[(11)C]methylation of corresponding precursors 1-[2-(3,5-bis-trifluoromethyl-benzyloxy)-1-phenyl-ethyl]-piperazine and {4-[2-(3,5-bis-trifluoromethyl-benzyloxy)-1-phenyl-ethyl]-piperazine-1-yl}-acetic acid using [(11)C]methyl triflate and isolated by solid-phase extraction (SPE) purification procedure with 40-55% radiochemical yields, decay corrected to end of bombardment, and a synthesis time of 15-20 min. The initial PET dynamic studies of the tracers [(11)C] and [(11)C] in rats were performed using an animal PET scanner, IndyPET-II, developed in our laboratory. The results show the tracer [(11)C]BMP had better uptake in the animal brain than the tracer [(11)C]BME and gave higher quality rat brain images. Blocking studies by intravenous coinjection of hot tracer [(11)C]BMP with cold drug BMP had no effect on [(11)C]BMP-PET rat brain imaging. Likewise, blocking studies by intravenous coinjection of hot tracer [(11)C]BME with cold drug BME also showed no effect on [(11)C]BME-PET rat brain imaging. These results suggest that the localization of [(11)C]BMP and [(11)C]BME in rat brain is mediated by nonspecific processes, and the visualization of [(11)C]BMP-PET and [(11)C]BME-PET on rat brain is related to nonspecific binding.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
LS7931102	3-(benzyloxy)-2,4-dichlorophenylboronic acid			Price

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