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A Homobivalent SPECT Radioligand ‐ Serinol Appended Methoxyphenyl Piperazine Derivative for Serotonin Receptor Imaging **
Author(s) -
Rangaswamy Sandhya,
Saklani Meenakshi,
Kumar Rajnish,
Mathur Rashi,
Kaul Ankur,
Tiwari Anjani K.,
KaurGhuman Sandeep,
Mishra Anil K.,
Varshney Raunak
Publication year - 2021
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.202100549
Subject(s) - radioligand , chemistry , piperazine , ligand (biochemistry) , serotonin , single photon emission computed tomography , spect imaging , 5 ht receptor , linker , stereochemistry , receptor , pharmacology , biophysics , neuroscience , biochemistry , psychology , nuclear medicine , biology , medicine , organic chemistry , computer science , operating system
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.