Authors:
Kakali De Indian Institute of Chemical Biology Department of Nuclear Medicine 4, Raja S.C. Mullick Road Kolkata 700 032 India

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Susmita Chandra Indian Institute of Chemical Biology Department of Nuclear Medicine 4, Raja S.C. Mullick Road Kolkata 700 032 India

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Bhart Sarkar Regional Radiation Medicine Centre, Thakurpukur Cancer Research Centre Kolkata 700 063 India

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Santanu Ganguly Regional Radiation Medicine Centre, Thakurpukur Cancer Research Centre Kolkata 700 063 India

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Mridula Misra Indian Institute of Chemical Biology Department of Nuclear Medicine 4, Raja S.C. Mullick Road Kolkata 700 032 India

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Abstract  

In the recent years interests on dihydropyrimidinone and their analogues have increased potentially due to their wide range of pharmacological/biological activities. Synthesis, radiolabeling with technetium-99 m (99mTc) and biological evaluation of 5-etoxycarbonyl-4-phenyl-6-methyl-3,4-dihydro-(1H)-pyrimidine-2-one (DHPM) were studied in this present work. After synthesis complexation of DHPM with 99mTc was carried out using stannous chloride as the reducing agent. The complex (99mTc-DHPM) was characterized by thin layer chromatography, radio-HPLC technique and determination of partition co-efficient. Radiochemical stability and particle size distribution of the complex were also measured. Biodistribution/scintigraphy studies were performed in rats and rabbits to evaluate the pharmacological characteristics of this complex. The radiochemical purity of the complex was over 95% as studied by thin layer chromatography and radio-HPLC. It was stable over 24 h at room temperature. Its partition coefficient indicated that it was a lipophilic complex. According to the European Pharmacopeia, >80% of 99mTc labeled radiopharmaceutical (99mTc-MAA) in the size range 10–50 μm, must be accumulated in the lungs 15 min after intravenous administration. In this study >85% of the 99mTc-DHPM complex in the average size of 40 μm. Biodistribution studies of 99mTc-DHPM in rat revealed that the complex accumulated in the lung with high uptake and good retention after intravenous administration. Scintigraphic studies in rabbit also revealed that most of the administered radiolabeled complex was accumulated in the lungs and after 1 h slowly excreted through the renal system. The lung uptake (ID%/g) was 10.12, 9.67, 8.60 and 5.01 and the lung/liver ratio was 7.49, 2.88, 2.62 and 1.87 at 2, 15, 30 and 60 min post-injection, respectively. These results suggested that 99mTc-DHPM could be suitable as a potential lung perfusion imaging agent. Further studies with 99mTc-DHPM and its derivatives are warranted to develop new 99mTc-labeled imaging agents for clinical applications.

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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)