Biological Evaluation and Binding Mechanism of 5-HT 7 Specific Arylpiperazinyl-Alkyl Benzothiazolone: Radiobiology and Photo-physical Studies.

Autor: Kumari N; Department of Chemistry, Babasaheb Bhimrao Ambedkar University, Uttar Pradesh, Lucknow, 226025, India.; CBRN Protection and decontamination research group, Division of Cyclotron and Radiological, Nuclear and Imaging Sciences, Institute of Nuclear Medicine and Allied Sciences, Timarpur, 110054, Delhi, India.; Department of Chemistry, Sri Venkateswara College, University of Delhi, Benito JuarezMarg, New Delhi, 110021, India., Singh D; Department of Chemistry, Babasaheb Bhimrao Ambedkar University, Uttar Pradesh, Lucknow, 226025, India., Singh P; Department of Chemistry, Babasaheb Bhimrao Ambedkar University, Uttar Pradesh, Lucknow, 226025, India., Mishra A; Department of Chemistry, Babasaheb Bhimrao Ambedkar University, Uttar Pradesh, Lucknow, 226025, India., Gond C; Department of Chemistry, Babasaheb Bhimrao Ambedkar University, Uttar Pradesh, Lucknow, 226025, India., Ojha H; CBRN Protection and decontamination research group, Division of Cyclotron and Radiological, Nuclear and Imaging Sciences, Institute of Nuclear Medicine and Allied Sciences, Timarpur, 110054, Delhi, India., Tiwari AK; Department of Chemistry, Babasaheb Bhimrao Ambedkar University, Uttar Pradesh, Lucknow, 226025, India. anjanik2003@gmail.com.
Jazyk: angličtina
Zdroj: Journal of fluorescence [J Fluoresc] 2024 Jan; Vol. 34 (1), pp. 341-352. Date of Electronic Publication: 2023 May 30.
DOI: 10.1007/s10895-023-03266-4
Abstrakt: Diversely substituted methoxy derivatives of arylpiperazinyl-alkyl benzothiazolone has been evaluated as specific probe for 5HT 7 . To determine the best methoxy derivative for 5HT 7 receptor affinity, we synthesised a number of 2-benzothiazolone arylalkyl piperazine derivatives. In-vitro/vivo studies with C-2 substituted [ 11 C]ABT showed 5HT 7 specific binding. The radiochemical purity of [ 11 C]ABT was found to be more than 99% with radiochemical stability persistence for more than 1.5 hr at 25 °C. The interaction of BSA and ABT has been analysed by photophysical studies for better understanding of properties such as adsortion, distribution, metabolism and elemination (ADME). The interaction between ABT and BSA was analyzed by using the UV-vis and fluorescence spectra. UV-vis spectra analyzed the changes in primary structure of BSA on its interaction with ABT. ABT showed quenched fluorescence emission intensity of tryptophan residues in BSA via static quenching mechanism. This study might help to understand how ABT binds to serum protein or subsequently to know the ADME of this drug candidate.
(© 2023. The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature.)
Databáze: MEDLINE