title: [PHARMACOLOGICAL STUDY OF NEW COMPOUNDS ACTING AS REGULATORS OF 18-KDA TRANSLOCATOR PROTEIN LIGANDS].
abstract: The interaction of new original 1-arylpyrrolo[1,2-a]pyrazine-3-carboxamide derivatives with mitochondrial translocator protein (MTP) 18 kDa has been studied by radioligand binding assay. Compounds GML-1 (Ki = 5.2 x 10⁻⁸ M) and GML-3 (Ki = 5.3 x 10⁻⁷ M) exhibit high binding affinity for MTP. GML-1 and GML-3 in a dose range of 0.1-1 mg/kg (i.p.) demonstrated anxiolytic-like effects in the elevated plus-maze test in CD-1 mice, which were blocked by the MTP selective antagonist PK11195. The data obtained on the molecular target, anxiolytic-like effects and low toxicity GML-1 and GML-3 suggest that these compounds are promising for further investigation as anxiolytics.
authors.forename: S A
authors.initials: SA
authors.lastname: Yarkov
authors.forename: G V
authors.initials: GV
authors.lastname: Mokrov
authors.forename: T A
authors.initials: TA
authors.lastname: Gudasheva
authors.forename: M A
authors.initials: MA
authors.lastname: Yarkova
authors.forename: S B
authors.initials: SB
authors.lastname: Seredenin
mesh_terms: D000818:Animals; D014151:Anti-Anxiety Agents / Q000737:chemistry / Q000494:pharmacology*; D002352:Carrier Proteins / Q000819:agonists* / Q000378:metabolism*; D007546:Isoquinolines / Q000737:chemistry / Q000494:pharmacology*; D018782:Maze Learning / Q000187:drug effects*; D051379:Mice
chemical_list: D014151:Anti-Anxiety Agents; D002352:Carrier Proteins; D007546:Isoquinolines; C106092:microsomal triglyceride transfer protein; C037850:PK 11195