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\begin{document}

\title{Improved Acetamidobenzoxazolone derivatised Radioligand for
Visualization of~ 18 kDa Translocator Protein and their comparison with
Luminescent nanoprobe~ of TSPO}



\author[1]{SRSTT Radiopharmaconnect}%
\affil[1]{Radiopharmaconnect}%


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  \date{March 14, 2025}


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\textbf{Authors:~ \textbf{Priya Singh}}, Deepika Singh, Anupriya
Adhikari, \textbf{\textbf{Anjani Kumar Tiwari*}}

Department of Applied Chemistry \& Nuclear Medicine, Babasaheb Bhimrao
Ambedkar Univerity, Lucknow, India 226025

\par\null

\textbf{Background}

In search of new ligand for ~translator protein (TSPO, 18 kDa) which is
a known inflammatory and oncological marker and present mainly on outer
surface of mitochondria in microglial cells of brain and other
peripheral organs such as kidney, lungs, liver, and spleen, a new
modified benzoxazolone has been synthesized and compared with
Luminescent nanoprobe of TSPO.

\emph{}

\textbf{Aims}

We have synthesised improved acetamidobenzoxazolone derivatised
radioprobe for visualization of 18 kDa TSPO which is able to overcome
the limitation of previous generation ligands as well as comparison of
sensitivity and specificity with TSPO specific nanoprobes.

\par\null

\textbf{Methods}

Computational analysis was performed by Glide, Schrodinger to designated
ligand. Reference molecules as well as nano probes were synthesised in
wet lab and characterized by different spectroscopic techniques. Mild
focal ischemia (MFI) produced by intraluminal occlusion of the middle
cerebral artery of SD rats by intraluminal thread model were used for
ARG and PET studies.

\par\null

\textbf{Results and Conclusion}

In conclusion, we demonstrated that our synthesized PET radioprobe
{[}\textsuperscript{11}C{]}N\textsubscript{e}BMP shows
radiopharmaceutical profile for imaging of PBR/TSPO expression during
neuroinflammation and comparable to nanoprobes . Further opti-mization
may lead to a new ligand for clinics for TSPO imaging having minimal
impact by TSPO rs6971.

\par\null

\textbf{References}

\textbf{1.} Fujinaga M. et al, Development of
a~\textsuperscript{18}F-labeled radioligand with improved brain kinetics
for positron emission tomography imaging of translocator protein~ (18
kDa)~ in ischemic brain and glioma. J Med Chem. 2017,~\textbf{60},
4047-4061.~

\textbf{2.} Tiwari A. K. et al, {[}\textsuperscript{18}F{]}FEBMP:
Positron Emission Tomography Imaging of TSPO in a Model of
Neuroinflammation in Rats, and in vitro Autoradiograms of the Human
Brain. Theranostics 2015,~\textbf{5}, 961-969.

\textbf{3.} Tiwari A. K. et al, Radiosynthesis and evaluation of
acetamidobenzoxazolone based radioligand
{[}\textsuperscript{11}C{]}N'-MPB for visualization of 18 kDa TSPO in
brain. New J. Chem., 2020,\textbf{44}, 7912-7922

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