Decrease in expression of α2a-adrenoreceptors in the brain of neonatal rats modulates exploratory behavior on the stage of its development

Reduction in α2A-adrenoreceptors (α2A-AR) expression in the rat brain during neonatal ontogenesis has been observed to influence neurochemical, hormonal, and behavioral characteristics on the stage of exploratory behavior development. Injection of antisense nucleotide complimentary to α2A-AR mRNA on the 2^nd–4^th day after birth has been demonstrated to decrease the quantity of α2-AR in the brain at this stage significantly. Subsequent increase in receptor’s expression (inhibited after the treatment) and its excess in the brainstem and hippocampus over the control meanings at 3 weeks of age were detected. Reduction in the basal corticosterone level in the blood and significant increase in exploratory behavior in the open-field test (number of risings on the hind legs) has been demonstrated in three-week-old pups. No differences in motor activity of these rats assessed by the number of grid crossings were indicated compared to control animals. In total, the reported results have been shown to indicate the presence of a deferred influence of short-term decrease in the brain α2A-AR expression in the first day of life on the subsequent development of α2A-AR system and exploratory behavior.     

Ribosomal tunnel and translation regulation

This review describes the results of recent studies of the ribosomal tunnel (RT), the major function of which is to allow the smooth passage of nascent polypeptides with different sequences from the peptidyl transferase center of the ribosome to the tunnel exit, where the folding of protein molecules begins. The features of structural organization of RT and their role in modulation and stabilization of the nascent chain conformation are discussed. Structural features of macrolide binding sites as well as application of macrolide antibiotics and their derivatives as tools to investigate ligand-tunnel wall interactions are also considered. Several examples of strong and specific interactions of regulatory polypeptides with nucleotide and amino acid residues of RT that lead to ribosome stalling and translational arrest are described in detail. The role of these events in regulation of expression of certain genes is discussed on the basis of recent high-resolution structural studies of nascent chains in the RT.     

In vivo efficacy of Ingavirin against pandemic A (H1N1/09)v influenza virus

Ingavirin was shown to be efficient in inhibition of the pandemic influenza virus strains A/California/04/2009 (H1N1)v, A/California/07/2009 (H1N1)v, A/Moscow/225/2009 (H1N1)v and A/Moscow/226/2009 (H1N1)v. as well as the influenza virus strain A/Aichi/2/68 (H3N2) in the lungs of the infected mice. After oral administration of Ingavirin the titers of the influenza virus strains in the lung homogenates lowered.     

Synthesis of heteroaromatic N-β-glycosides of N-acetylglucosamine under the conditions of phase transfer catalysis: I. Glucosaminides of 2-oxobenzazoles

Glycosylation of benzothiazolone-2, 5-methylbenzoxazolone-2, and benzothiazolone-2 with the full acetate of α-D-glucosaminyl chloride in the phase transfer systems investigated (solid-organic solvent and aqueous alkali-organic solvent) regioselectively leads to the corresponding N-β-D-glucosaminides, which is proved by ¹H NMR spectroscopy and X-ray analysis.     

Effect of intramolecular interactions on circular dichroism of ortho-substituted 1-phenethylamines

The synthesis of ortho-substituted (S)-1-phenethylamines via ortho-lithiation of its N,N-dimethyl derivative followed by reactions with different reagents is described. Circular dichroism spectra of synthesized compounds were measured. It is shown that the observed short-wave Cotton effects greatly depend on the existence of cyclic structure due to possible interactions such as hydrogen bond or electrostatic interaction.     

Subtype-specific clinically important effects of alpha 2-adrenergic receptors

A- B- and C-subtypes of alpha 2-adrenoreceptors present in all mammals are involved in responses to currently existing subtype-nonselective ligands of these receptors widely used in medicine. Each of the subtypes has its own specific distribution in tissue and cells, onthogenetic pattern, specific regulation of activity and expression, and, as result, specific physiological functions. The latter suggests opportunities of using the subtype-specific for correction of the functions depending on this receptor. The article reviews the role of individual subtypes of alpha 2-adrenoreceptors in regulation of neurochemical transmission of cardiovascular system, psychoemotional state and development of psychic disorders, and also male sexual behaviour.