The first dipeptide ligand of translocator protein: Design and anxiolytic activity
| Autor: | M. A. Yarkova, Tatiana A Gudasheva, G. V. Mokrov, O. A. Deeva, S. B. Seredenin, Yarkov Sa |
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| Rok vydání: | 2015 |
| Předmět: |
Male
Elevated plus maze Stereochemistry medicine.drug_class Drug Evaluation Preclinical Biophysics Anxiety Motor Activity Ligands Biochemistry Anxiolytic Pyrazolopyrimidine chemistry.chemical_compound Receptors GABA Animals Outbred Strains medicine Translocator protein Animals Maze Learning Mice Inbred BALB C Dipeptide Dose-Response Relationship Drug Molecular Structure biology Chemistry Ligand Dipeptides General Chemistry General Medicine Isoquinolines Anti-Anxiety Agents Alpidem Mechanism of action Drug Design Exploratory Behavior biology.protein medicine.symptom Central Nervous System Agents medicine.drug |
| Zdroj: | Doklady Biochemistry and Biophysics. 464:290-293 |
| ISSN: | 1608-3091 1607-6729 |
| Popis: | On the basis of the structure of Alpidem, a pyrazolopyrimidine ligand of the translocator protein (TSPO), a dipeptide TSPO ligand, N-carbobenzoxy-L-tryptophanyl-L-isoleucine amide (GD-23), was designed and synthesized using our own original peptide design strategy. This compound exhibited anxiolytic activity in BALB/cAnN mice in the "open-field" test and in outbred CD1 mice in the "elevated plus maze" test. The stereoselectivity of the anxiolytic effect of GD-23 is demonstrated. The results of this study suggest that GD-23 is a ligand of the translocator protein, and its structure can become the basis for creating anxiolytics with a fundamentally new mechanism of action. |
| Databáze: | OpenAIRE |
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