New, eco-friendly method for synthesis of 3-chlorophenyl and 1,1'-biphenyl piperazinylhexyl trazodone analogues with dual 5-HT1A/5-HT7 affinity and its antidepressant-like activity

Serotonin 5-HT(1A) and 5-HT(7) receptors play an important role in the pathogenesis and pharmacotherapy of depression. Previously identified N-hexyl trazodone derivatives, 2-(6-(4-(3-chlorophenyl)piperazin-1-yl)hexyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one hydrochloride (7a·HCl), with high affinity for 5-HT(1A)R and 2-(6-(4-([1,1′-biphenyl]-2-yl)piperazin-1-yl)hexyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one hydrochloride (7b·HCl), a dual-acting 5-HT(1A)/5-HT(7) receptor ligand, were prepared with a new microwave-assisted method. The protocol for the synthesis of 7a and 7b involved reductive alkylation under a mild reducing agent. We produced the final compounds with yield of 56–63% using ethanol or 51–56% in solvent-free conditions in 4 min. We then determined the 5-HT(7)R binding mode for compounds 7a and 7b using in silico methods and assessed the preliminary ADME and safety properties (hepatotoxicity and CYP3A4 inhibition) using in vitro methods for 7a·HCl and 7b·HCl. Furthermore, we evaluated antidepressant-like activity of the dual antagonist of 5-HT(1A)/5-HT(7) receptors (7b·HCl) in the forced swim test (FST) in mice. The 5-HT(1A)R ligand (7a·HCl) with a much lower affinity for 5-HT(7)R compared to that of 7b·HCl was tested comparatively. Both compounds showed antidepressant activity, while 5-HT(1A)/5-HT(7) double antagonist 7b·HCl showed a stronger and more specific response

Search report of meteorites in Oslo

A piece of a meteorite that had crashed through the roof of a cottage house was find in the central Oslo quarter Rodelřkka at the beginning of March 2012. Some days later the second discovery in the melting snow of Ekebergsletta hilltop plateau triggered the hunting for meteorites in almost all sides of Oslo. The pieces of third meteorite broken by cars and spread out by snowplow was discovered on the asphalt road side by Maciek Burski, the member of Polish Meteoritical Society. Later on the missing fragments of the Maciek’s most east find was collected by Meteoritical Section members of Comet and Meteor Workshop (PKiM) with the help of local meteoritical authorities. The total mass of this unobserved fall is 6.22 kg in five pieces spread out in the eight km-long strewnfield with 200 g and 4.65 kg meteorites on the opposite ends. The Meteorite is not classified yet but unofficial information is “breccia H3-4”

Early Complications of Radioisotope Therapy with Lutetium-177 and Yttrium-90 in Patients with Neuroendocrine Neoplasms—A Preliminary Study

Neuroendocrine neoplasms (NENs) constitute a heterogenous group of tumors originating from neuroendocrine cells scattered throughout the body. Peptide Receptor Radionuclide Therapy (PRRT) is a treatment of choice of unresectable metastasized progressive and well-differentiated NENs. The aim of the study was to assess early bone marrow and kidney injury after administration of Lutetium-177 or Lutetium-177 combined with Yttrium-90. Thirty-one patients received treatment with [177Lu]Lu-DOTATATE with the activity of 7.4 GBq. Eleven patients received tandem treatment with [90Y]Y-DOTATATE with the activity of 1.85 GBq + [177Lu]Lu-DOTATATE with the activity of 1.85 GBq. After PRRT a significant decrease in leukocyte, neutrophil, and lymphocyte counts was noted. Tandem treatment demonstrated a more marked decrease in white blood cell count compared to Lutetium-177 therapy only. Conversely, no significant influence on glomerular filtration was found in this assessment. However, PRRT triggered acute renal tubule dysfunction, regardless of the treatment type. Regarding the acute complications, PRRT appeared to be a safe modality in the treatment of patients with NEN

Report on meteorite field search within PFN in 2016/2017 season

The Meteorite Section was created in 2010 on demand of Polish Fireball Network (PFN) for the meteorite searching and investigation purposes. The main task of the Section is to find the meteorites dropped from bolides registered by the Polish Fireball Network. Each year, the PFN registers several meteorite falls within our country and meteorite strewnfield inspections must be carried out at least for the masses of above 300 g estimated with the PyFN software. Only last year the PFN organized several search campaigns. Two of them are presented in the publication

15 years of observation – selected meteorite falls registered in the PFN in 2004–2019

The Polish Fireball Network (PFN) associated in Comets and Meteors Workshop monitors the sky over Poland regularly for 15 years and registers the bright fireballs over the whole country (Olech 2006; Wiśniewski 2017). Every year we observe a few meteorite falls but due to weather conditions some data are not sufficient for proper strewnfield calculations. In the collaboration with the European Fireball Network the whole territory of Poland is monitored almost regardless of the weather. The publication describes the bolide phenomena characterized by distinctive meteorite falls, so the strewnfield indicated here should become the target of further exploration expeditions

Preliminary characteristic of water chemistry of lake Bartąg near Olsztyn and sketch of its protection concept

Badania prowadzono na jeziorze Bartąg (powierzchnia 72,3 ha, max. głębokość 15,2 m) pod Olsztynem. Zlewnia jeziora ma powierzchnię 400,3 ha, w której największy udział mają grunty orne – 68,9%, lasy zajmują 19,7%, a teren zabudowany – 11,4%. W wodach jeziora stwierdzono jednostkowe i duże ilości biogenów, sięgające 1,24 mg Pog.∙dm–3 i 2,35 mg Nog.∙dm–3 oraz wapnia – 61,0 mg Ca∙dm–3. Przyczyną dużej trofii tego zbiornika jest nadmierne jego obciążenie biogenami spływającymi ze zlewni. Rzeczywiste ładunki biogenów spływające do jeziora przekraczają wartości krytyczne obliczone wg Vollenweidera. Niska jakość wód tego jeziora, z jednoczesnym dużym obciążeniem ładunkiem zanieczyszczeń, ze zlewni wskazuje na konieczność podjęcia działań ochronnych, polegających na zmniejszeniu obciążenia zewnętrznego.The study was carried out on Lake Bartąg (area 72.3 ha, maximum depth 15.2 m) near Olsztyn. The catchment area of the lake is 400.3 ha, in which arable land cover the largest share – 68.9%, forests occupy 19.7%, and built-up area – 11.4%. In the lake's waters, unitary and large amounts of nutrients were found, reaching 1.24 mg TP∙dm–3 and 2.35 mg TN∙dm–3 and calcium – 61.0 mg Ca∙dm–3. The reason for the high trophic status of this reservoir is its excessive load on biogenes flowing from the drainage basin. The actual loads of nutrients flowing into the lake exceed the critical values calculated according to Vollenweider. The low quality of the lake's waters, with a heavy load of pollutants, from the catchment points to the need to take protective measures, which consist in reducing the external load