Design,Synthesis, and Biological Evaluation of Catecholamine Vehicle for Studying Dopaminergic System |
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Authors: | Pooja Singh Vikas Kumar Swati Aggarwal Anjani K Tiwari Krishna Chuttani Ramendra Pratap Anil K Mishra |
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Institution: | 1. Division of Cyclotron and Radiopharmaceutical Sciences, Institute of Nuclear Medicine and Allied Sciences, , Delhi, 110054 India;2. Department of Chemistry, University of Delhi, , Delhi, 110007 India;3. Department of Zoology, University of Delhi, , Delhi, 110007 India |
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Abstract: | Catecholamine mimetic EDTA‐bis(tyramide) was synthesized and characterized by various spectroscopic techniques (NMR, mass spectroscopy) and λem 310 nm for the excitation at 270 nm. Molecular docking studies were performed with human serum albumin (PDB 1E78), showing binding pattern with amino acid residues Arg218, Arg222, and Lys444, identifies the ligand‐human serum albumin interaction for the transportation affinity of the ligand at the specific site of the target. Subsequently, binding study with human serum albumin at λex = 350 nm found to be 5.847 × 104 m ?1 shows effective quenching effect. Additionally, to go more insight, acetylcholinesterase binding affinity was investigated, which shows 90% binding affinity for the 10 mm concentration. IC50 value was found 18.60 μm for MAO‐B inhibition. Finally, EDTA‐bis(tyramide) labeled with 99mTc to investigate its in vivo radiopharmaceutical efficiency having 97% binding affinity with 98% radiochemical purity. In vivo studies were carried out for 99mTc‐EDTA‐bis(tyramide) included blood kinetics showed a quick wash out from the circulation via renal route, and biodistribution revealed that maximum %ID/g was found in kidney at 1 h, and its scintigraphy image shows 3.96% brain uptake with respect to whole body. |
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Keywords: | 99mTc labeling AChE brain imaging EDTA‐bis(tyramide) human serum albumin |
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