[PHARMACOLOGICAL STUDY OF NEW COMPOUNDS ACTING AS REGULATORS OF 18-KDA TRANSLOCATOR PROTEIN LIGANDS].

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.

The first dipeptide ligand of translocator protein: Design and anxiolytic activity.

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 Novel Dipeptide Translocator Protein Ligand, Referred to As GD-23, Exerts Anxiolytic and Nootropic Activities.

The translocator protein (TSPO) promotes the translocation of cholesterol to the inner mitochondrial membrane and mediates steroid formation. In this study, we first report on a biological evaluation of the dipeptide GD-23 (N-carbobenzoxy-L tryptophanyl-L isoleucine amide), a structural analogue of Alpidem, the principal TSPO ligand. We show that GD-23 in a dose range of 0.

Design, synthesis and anxiolytic-like activity of 1-arylpyrrolo[1,2-a]pyrazine-3-carboxamides.

A series of 1-arylpyrrolo[1,2-a]pyrazine-3-carboxamides were designed and synthesized as 18kDa translocator protein (TSPO) ligands. Anxiolytic-like activity of compounds was evaluated in the open field test and elevated plus maze test. Compounds 1a and 1b demonstrated high anxiolytic-like effect in the dose range of 0.

Development of liposome immune lysis assay for the herbicide atrazine.

A homogeneous complement-mediated liposome immune lysis assay (LILA) was developed for determination of the herbicide atrazine. To dispose the antigen on the surface of lipid bilayer the atrazine was conjugated to a dimirystoylphosphatidylethanolamine (DMPE) carrier. Calcein was compared with sulforhodamine 101 as a fluorophore label for entrapping into the antigen-sensitized liposomes.