Synthesis and Biological Evaluation of 99mTc-DHPM Complex: a Potential new Radiopharmaceutical for Lung Imaging Studies
IR@IICB: CSIR-Indian Institute of Chemical Biology, Kolkata
View Archive Info| Field | Value | |
| Title |
Synthesis and Biological Evaluation of 99mTc-DHPM Complex:
a Potential new Radiopharmaceutical for Lung Imaging Studies
|
|
| Creator |
De, Kakali
Chandra, Susmita Sarkar, Bhart Ganguly, Santanu Misra, Mridula |
|
| Subject |
Infectious Diseases and Immunology
|
|
| Description |
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 lm, 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 lm. 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.
|
|
| Date |
2010
|
|
| Type |
Article
PeerReviewed |
|
| Format |
application/pdf
|
|
| Identifier |
http://www.eprints.iicb.res.in/50/1/JOURNAL_OF_RADIOANALYTICAL_AND_NUCLEAR_CHEMISTRY___283(_3)_;2010[110].pdf
De, Kakali and Chandra, Susmita and Sarkar, Bhart and Ganguly, Santanu and Misra, Mridula (2010) Synthesis and Biological Evaluation of 99mTc-DHPM Complex: a Potential new Radiopharmaceutical for Lung Imaging Studies. Journal of Radioanalytical and Nuclear Chemistry, 283. pp. 621-628. |
|
| Relation |
http://dx.doi.org/:10.1186/1476-4598-9-58
http://www.eprints.iicb.res.in/50/ |
|