Dipeptide Ligands of TSPO

Our own investigations of the synthesis and pharmacological properties of dipeptide ligands of the translocator protein (TSPO) are reviewed. The compounds were designed based on the original chemical and pharmacological strategy of designing short peptides that are similar to known drugs. Two series...

Full description

Saved in:
Bibliographic Details
Published inPharmaceutical chemistry journal Vol. 56; no. 9; pp. 1169 - 1178
Main Authors Deeva, O. A., Yarkova, M. A., Mokrov, G. V., Gudasheva, T. A., Seredenin, S. B.
Format Journal Article
LanguageEnglish
Published New York Springer US 01.12.2022
Springer
Subjects
Amino acids
Antianxiety agents
Medicine
Organic Chemistry
Peptides
Pharmacology/Toxicology
Pharmacy
Search for New Drugs
dipeptides
TSPO ligands
anxiolytic activity
design
pharmacological inhibitory assay
Online AccessGet full text

Cover

More Information
Summary:Our own investigations of the synthesis and pharmacological properties of dipeptide ligands of the translocator protein (TSPO) are reviewed. The compounds were designed based on the original chemical and pharmacological strategy of designing short peptides that are similar to known drugs. Two series of TSPO dipeptide ligands, substituted tryptophanyl isoleucines and substituted tryptophanyl leucines, were designed and synthesized. Data for their anxiolytic activities, the proposed molecular mechanisms of action of the lead compounds, and the structure—activity (anxiolytic) relationship of their analogs are presented. The pharmacophore elements necessary for the manifestation of the anxiolytic effects of these compounds are described. A hypothesis about the structure of the putative endogenous TSPO ligand is formulated.
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-022-02772-2