Preparation of 99mTc-PQQ and preliminary biological evaluation for the NMDA receptor

Yanyan Kong; Xingqin Zhou; Guoxian Cao; Xijie Xu; Meifen Zou; Xiaofeng Qin; Rongjun Zhang

doi:10.1007/s10967-010-0845-5

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Journal of Radioanalytical and Nuclear Chemistry

Volume/Issue:: Volume 287: Issue 1

Preparation of ^99mTc-PQQ and preliminary biological evaluation for the NMDA receptor

Authors:

Yanyan Kong

Yanyan Kong Department of Nuclear Medicine, Huashan Hospital, Fudan University, Shanghai, 200040 China

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Xingqin Zhou

Xingqin Zhou Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi, Jiangsu 214063, China

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Guoxian Cao

Guoxian Cao Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi, Jiangsu 214063, China

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Xijie Xu

Xijie Xu Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi, Jiangsu 214063, China

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Meifen Zou

Meifen Zou Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi, Jiangsu 214063, China

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Xiaofeng Qin

Xiaofeng Qin Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi, Jiangsu 214063, China

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, and

Rongjun Zhang

Rongjun Zhang Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi, Jiangsu 214063, China

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Pages:: 93–101

Online Publication Date:: 09 Oct 2010

Publication Date:: 01 Jan 2011

Article Category:: Research Article

DOI:: https://doi.org/10.1007/s10967-010-0845-5

Keywords:: Pyrroloquinoline quinone; 99mTc; 99mTc-PQQ; NMDAR

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Abstract

Pyrroloquinoline quinone (PQQ), an essential nutrient, antioxidant, redox modulator and nerve growth factor found in a class of enzymes called quinoproteins, was labeled with ^99mTc by using stannous fluoride (SnF₂) method. Radiolabeling qualification, quality control and characterization of ^99mTc-PQQ and its biodistribution studies in mice were performed and discussed. Effects of pH values, temperature, time and reducing agents concentration on the radiolabeling yield were investigated. The quality control procedure of ^99mTc-PQQ was determined by thin layer chromatography (TLC), radio high-performance liquid chromatography (RHPLC) and paper electrophoresis methods. The average radiolabeling yield was 94 ± 1% under optimum conditions of 0.99 mg of PQQ, 30 μg of SnF₂, 0.5 mg of ethylenediaminetetraacetic acid disodium salt (EDTA-2Na) and 18.5 MBq of Na^99mTcO₄ at pH 6 and 25 °C with a response volume of 1 ± 0.1 mL. ^99mTc-PQQ was stable and anionic. Lipid–water partition coefficient of ^99mTc-PQQ was −1.49 ± 0.16. The pharmacokinetics parameters of ^99mTc-PQQ were t_1/2α = 18.16 min, t_1/2β = 100.45 min, K₁₂ = 0.013 min⁻¹, K₂₁ = 0.017 min⁻¹, K_e = 0.016 min⁻¹, AUC (area under the curve) = 1040.78 ID% g⁻¹ min and CL (plasma clearance) = 0.096 mL min⁻¹. The dual-exponential equation was Y = 10.88e^−0.038t + 5.21e^−0.0069t. The biodistribution of ^99mTc-PQQ was studied in ICR (Institute for Cancer Research 7701 Burhelme Are., Fox Chase, Philadelphia, PA 1911 USA) mice. In vitro autoradiographic studies clearly showed that the ^99mTc-PQQ radioactivity accumulated predominantly in the hippocampus and cortex, which had a high density of N-methyl-d-aspartate Receptor (NMDAR). The enrichment can be blocked by NMDAR redox modulatory site antagonists-ebselen (EB) and ^99mTc-PQQ is therefore a promising candidate for the molecular imaging of NMDAR. To date, however, there have been no studies characterizing ^99mTc-PQQ.

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Journal of Radioanalytical and Nuclear Chemistry

Print ISSN:: 0236-5731

Online ISSN:: 1588-2780

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Journal of Radionalytical and Nuclear Chemistry
Language	English
Size	A4
Year of Foundation	1968
Volumes per Year	1
Issues per Year	12
Founder	Akadémiai Kiadó
Founder's Address	H-1117 Budapest, Hungary 1516 Budapest, PO Box 245.
Publisher	Akadémiai Kiadó Springer Nature Switzerland AG
Publisher's Address	H-1117 Budapest, Hungary 1516 Budapest, PO Box 245. CH-6330 Cham, Switzerland Gewerbestrasse 11.
Responsible Publisher	Chief Executive Officer, Akadémiai Kiadó
ISSN	0236-5731 (Print)
ISSN	1588-2780 (Online)