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- Title
Design, Synthesis, and Biological Evaluation of Catecholamine Vehicle for Studying Dopaminergic System.
- Authors
Singh, Pooja; Kumar, Vikas; Aggarwal, Swati; Tiwari, Anjani K.; Chuttani, Krishna; Pratap, Ramendra; Mishra, Anil K.
- 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 1 E78), 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 m m concentration. IC50 value was found 18.60 μ m for MAO-B inhibition. Finally, EDTA-bis(tyramide) labeled with 99m Tc to investigate its in vivo radiopharmaceutical efficiency having 97% binding affinity with 98% radiochemical purity. In vivo studies were carried out for 99m Tc- 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.
- Subjects
CATECHOLAMINES; DOPAMINERGIC mechanisms; ETHYLENEDIAMINETETRAACETIC acid; MASS spectrometry; NUCLEAR magnetic resonance; AMINO acids; RADIOPHARMACEUTICALS
- Publication
Chemical Biology & Drug Design, 2013, Vol 82, Issue 2, p226
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.12147