Development of new radiopharmaceuticals for nuclear brain imaging: pharmacokinetics and mechanism of action
IR@IICB: CSIR-Indian Institute of Chemical Biology, Kolkata
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| Title |
Development of new radiopharmaceuticals for nuclear brain imaging: pharmacokinetics and mechanism of action
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| Creator |
Chandra, Susmita
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| Subject |
Drug Development/Diagnostics & Biotechnology
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| Description |
The tripeptide, NH2PhePheCys was synthesized with a very high yield (> 95%), but
the oxidized form was synthesized with only 85% yield. The peptides were analytically
characterized by TLC, HPLC, NMR and Mass spectrometry. After radiolabeling the
complexation efficiency was found to be in the range of 90-95%. Octanol/buffer partition
coefficient showed that the complexes are quite lipophilic in nature. During biodistribution
significant uptake of 99mTc-NH2PhePheCys was observed in rat brain. The uptake in bone
marrow, liver, lung and spleen was also significant. 99mTc-NH2PhePheCys was cleared very
rapidly from blood and non-target tissues. Images with 99mTc-NH2PhePheCys in rabbit
under gamma camera showed similar biological characteristics as observed during
biodistribution studies in rat. In vivo metabolized form of 99mTc-NH2PhePheCys was
identified by HPLC studies of brain and liver homogenate of rat. In vivo stability of 99mTc-
NH2PhePheCys has been confirmed by performing HPLC of the urine sample.
Autoradiography of the normal and ischemic rat brain showed a clear differential uptake of
99mTc-NH2PhePheCys in normal and necrotic regions.
Results of the above study shows that the new radiopharmaceutical 99mTc-
NH2PhePheCys, which can be transported into the brain by a receptor mediated pathway
possesses a very high potential for various applications in the field of nuclear medicine,
specially in diagnosing various diseases of brain.
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| Date |
2009
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| Type |
Thesis
NonPeerReviewed |
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| Format |
application/pdf
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| Identifier |
http://www.eprints.iicb.res.in/12/1/Thesis_Susmita_2009_PDF.pdf
Chandra, Susmita (2009) Development of new radiopharmaceuticals for nuclear brain imaging: pharmacokinetics and mechanism of action. PhD thesis, Jadavpur University. |
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| Relation |
http://www.eprints.iicb.res.in/12/
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