| Title: |
A Homobivalent SPECT Radioligand ‐ Serinol Appended Methoxyphenyl Piperazine Derivative for Serotonin Receptor Imaging** |
| Authors: |
Rangaswamy, Sandhya; Saklani, Meenakshi; Kumar, Rajnish; Mathur, Rashi; Kaul, Ankur; Tiwari, Anjani K.; Kaur‐Ghuman, Sandeep; Mishra, Anil K.; Varshney, Raunak |
| Contributors: |
Defence Research and Development Organisation |
| Source: |
ChemistrySelect ; volume 6, issue 23, page 5670-5677 ; ISSN 2365-6549 2365-6549 |
| Publisher Information: |
Wiley |
| Publication Year: |
2021 |
| Collection: |
Wiley Online Library (Open Access Articles via Crossref) |
| Description: |
Serotonin receptor subtypes are predominantly accountable for various neurophysiologic and cognitive processes and are expressed in the hippocampus region. SPECT based radioligands offer a cost effective understanding to the molecular changes which are used in the diagnoses of various neurological disorders. A Homobivalent approach was used to synthesize 1‐(2‐methoxyphenyl) piperazine based ligand by using click chemistry to incorporate two moieties of MPP via a linker (serinol) for SPECT (Single Photon Emission Computerised Tomography) evaluation. Molecular docking studies show better affinity for radiolabeled DO3 A‐serinol‐bis‐MPP complex. The radiolabeling efficiency of conjugate was optimized and evaluated for stability by various parameters and was found to be 99 %. The complex shows appreciable brain uptake in rabbit. Ex Vivo pharmacology indicated approximately 50 % of the total brain uptake in the hippocampus region which showed the selective preference of the ligand for serotonin receptor. This study could be considered as a novel, informative and preclinical finding for using the synthesised 99m Tc‐DO3 A‐serinol‐bis‐MPP ligand to target serotonin receptor by SPECT imaging. |
| Document Type: |
article in journal/newspaper |
| Language: |
English |
| DOI: |
10.1002/slct.202100549 |
| Availability: |
https://doi.org/10.1002/slct.202100549; https://onlinelibrary.wiley.com/doi/pdf/10.1002/slct.202100549; https://onlinelibrary.wiley.com/doi/full-xml/10.1002/slct.202100549 |
| Rights: |
http://onlinelibrary.wiley.com/termsAndConditions#vor |
| Accession Number: |
edsbas.9B91342E |
| Database: |
BASE |