Influence of Diazepino [1,2-a] benzimidazole derivative (DAB-19) on behavioral aspects of animals

In the present study, compound DAB-19 was screened for its influence on animals` behavior patterns, such as aggression, obsessive-compulsive behavior, emotional lability, and unsociabilit

Searching for novel antagonists of adenosine A1 receptors among azolo[1,5-a]pyrimidine nitro derivatives

Introduction: Ligands of adenosine A1Rs are potential candidates for the development of drugs for the treatment of paroxysmal supraventricular tachycardia, angina pectoris, hypertriglyceridemia, type 2 diabetes mellitus, neuropathic pain, and heart failure. At the same time, there is a deficiency of drugs that can regulate the functions of A1 receptors. A number of A1-antagonists are at the various stages of clinical trials; other drugs are not very selective or are characterized by an insufficient breadth of their therapeutic action. Therefore, the search for new medicinal compounds for the prevention and treatment of A1-depended diseases among nitro derivatives of tetrazolo[1,5-a]pyrimidine and 1,2,4-triazolo[1,5-a]pyrimidine is of scientific interest. Materials and methods: The search for active compounds was carried out by in silico and in vitro methods. At the first stage, a computer forecast of A1-antagonistic activity was carried out using the Microcosm BioS software. At the second stage, the prediction results were verified in vitro in a model of isolated mouse atria. Results and discussion: Based on the results of the prediction by the method of maximum similarity to standards, the most active compounds III, VIII, and XVII were selected. After testing the prediction results by the isolated atria method, the compound VIII was characterized by A1-blocking effect in vitro at a concentration of 10 μmol/L. Conclusion: The most promising compound with A1-blocking effect in vitro was identified; it is a derivative of tetrazolo[1,5-a]pyrimidine under the code of VIII. It is of interest for us for further in-depth study of its pharmacological properties. Copyright Yakovlev DS et al.The reported study was partially funded by the Gover

Quantifying the photothermal conversion efficiency of plasmonic nanoparticles by means of terahertz radiation

© 2019 Author(s). The accurate determination of the photothermal response of nanomaterials represents an essential aspect in many fields, such as nanomedicine. Specifically, photothermal cancer therapies rely on the precise knowledge of the light-to-heat transfer properties of plasmonic nanoparticles to achieve the desired temperature-induced effects in biological tissues. In this work, we present a novel method for the quantification of the photothermal effect exhibited by nanoparticles in aqueous dispersions. By combining the spatial and temporal thermal dynamics acquired at terahertz frequencies, the photothermal conversion efficiency associated with the geometry of the plasmonic nanoparticles can be retrieved in a noncontact and noninvasive manner. The proposed technique can be extended to the characterization of all those nanomaterials which feature a temperature-dependent variation of the refractive index in the terahertz regime

Quantifying the photothermal conversion efficiency of plasmonic nanoparticles by means of terahertz radiation

© 2019 Author(s). The accurate determination of the photothermal response of nanomaterials represents an essential aspect in many fields, such as nanomedicine. Specifically, photothermal cancer therapies rely on the precise knowledge of the light-to-heat transfer properties of plasmonic nanoparticles to achieve the desired temperature-induced effects in biological tissues. In this work, we present a novel method for the quantification of the photothermal effect exhibited by nanoparticles in aqueous dispersions. By combining the spatial and temporal thermal dynamics acquired at terahertz frequencies, the photothermal conversion efficiency associated with the geometry of the plasmonic nanoparticles can be retrieved in a noncontact and noninvasive manner. The proposed technique can be extended to the characterization of all those nanomaterials which feature a temperature-dependent variation of the refractive index in the terahertz regime