Defect structure in δ-Bi5PbY2O11.5

A detailed study of the defect structure in a di-substituted δ-Bi₂O₃ type phase, δ-Bi₅PbY₂O_11.5, is presented. Using a combination of conventional Rietveld analysis of neutron diffraction data, reverse Monte Carlo (RMC) analysis of total neutron scattering data and ab initio molecular dynamics (MD) simulations, both average and local structures have been characterized. δ-Bi₅PbY₂O_11.5 represents a model system for the highly conducting δ-Bi₂O₃ type phases, in which there is a higher nominal vacancy concentration than in the unsubstituted parent compound. Uniquely, the methodology developed in this study has afforded the opportunity to study both oxide-ion vacancy ordering as well as specific cation–cation interactions. Oxide-ion vacancies in this system have been found to show a preference for association with Pb²⁺ cations, with some evidence for clustering of these cations. The system shows a non-random distribution of vacancy pair alignments, with a preference for 〈100〉 ordering, the extent of which shows thermal variation. MD simulations indicate a predominance of oxide-ion jumps in the 〈100〉 direction.

Total neutron scattering analysis and ab initio MD simulations reveal details of oxide ion vacancy ordering and migration pathways.     

Oral health of Polish three-year-olds and mothers' oral health-related knowledge

OBJECTIVES: To evaluate the oral health of Polish three-year-olds, to investigate oral health-related knowledge, habits and educational levels of their mothers, and to determine whether mothers' health-related knowledge influenced caries severity in their children. DESIGN: A cross-sectional. nationwide oral health survey of three-year-olds was performed in 2002. Their mothers completed self-administered questionnaires. PARTICIPANTS: The oral health survey covered 1,114 three-year-olds chosen by stratified random sampling. OUTCOME MEASURES: Dental caries was recorded according to WHO criteria and methods. Questionnaires investigated demographic factors, mothers' and children's oral health-related habits and oral health knowledge. RESULTS: A total of 43.8% of three-year-olds were caries-free. Mean dmft was 2.9, with the greatest component being decayed teeth (2.8). Nearly two-thirds of mothers had never taken their child to a dentist; a similar proportion declared care of the deciduous teeth to be unnecessary. Mothers' opinions concerning their children's oral health was over-optimistic. A strong interdependence was found between oral health and mothers' level of oral health-related knowledge, and between mothers' level of knowledge and their level of education. CONCLUSION: The level of dental caries in Polish three-year-olds was alarmingly high, and was associated with a low level of oral health-related knowledge among mothers, suggesting an urgent need for the implementation of systematic oral health education and promotion for expectant mothers and mothers of small children.     

Anatomical classification of the shape and topography of the stomach

The aim of the study was to present the classification of anatomical variations of the stomach, based on the radiological and historical data. In years 2006–2010, 2,034 examinations of the upper digestive tract were performed. Normal stomach anatomy or different variations of the organ shape and/or topography without any organic radiologically detectable gastric lesions were revealed in 568 and 821 cases, respectively. Five primary groups were established: abnormal position along longitudinal (I) and horizontal axis (II), as well as abnormal shape (III) and stomach connections (IV) or mixed forms (V). The first group contains abnormalities most commonly observed among examined patients such as stomach rotation and translocation to the chest cavity, including sliding, paraesophageal, mixed-form and upside-down hiatal diaphragmatic hernias, as well as short esophagus, and the other diaphragmatic hernias, that were not found in the evaluated population. The second group includes the stomach cascade. The third and fourth groups comprise developmental variations and organ malformations that were not observed in evaluated patients. The last group (V) encloses mixed forms that connect two or more previous variations.     

Synthesis and anticonvulsant activity of novel 2,6-diketopiperazine derivatives. Part 1: perhydropyrrole[1,2-a]pyrazines

A number of novel pyrrole[1,2-a]pyrazine derivatives were synthesized and evaluated in in vivo animal models of epilepsy. Among them, several compounds displayed promising seizure protection in the maximal electroshock seizure (MES), subcutaneous metrazol seizure (scMET), 6 Hz and pilocarpine-induced status prevention (PISP) tests, with ED₅₀ values comparable to the reference anticonvulsant drugs (AEDs). A critical influence of the stereochemistry and conformational preferences of the pyrrole[1,2-a]pyrazine core on in vivo pharmacological activity was observed. The mechanism of the anticonvulsant action of the agents synthesized is most probably not via inhibition of the voltage-dependent sodium (Na⁺) currents.     

Coffee and caffeine - enemies or alliantes of a cardiologist?

Caffeine is a widespread known psychoactive substance that is present mainly in coffee, tea, soft and energy drinks. As a natural methylopxanthine it blocks A1 and A2 adenosine receptors and in high doses inhibits the phosphodiesterase activity. Caffeine also decreases calcium ion accumulation in the mitochondria of cardiomyocytes. A clinical and experimental data indicates that the caffeine and coffee increase the arterial wall stiffness, blood pressure and endothelium-dependent flow mediated dilatation. Caffeine also elevates cholesterol and homocysteine blood level. Moderate coffee consumption decreases the mortality of the cardiac infarct. However, acceleration of acute ischemic cardiac disease correlates with high coffee intake. The metyloxantine easily crosses the blood-placenta barrier, and may induce intrauterine growth retardation. Due to chronotropic and inotropic activity it may induce fetal tachycardia and/or extrasystolic beats.     

Efficacy of indapamide SR compared with enalapril in elderly hypertensive patients with type 2 diabetes

BACKGROUND: Blood pressure control is the main influential variable in reducing microalbuminuria in patients with type 2 diabetes. In this subanalysis of the Natrilix SR versus Enalapril Study in hypertensive Type 2 diabetics with micrOalbuminuRia (NESTOR) study, we have compared the effectiveness of indapamide sustained release (SR) and enalapril in reducing blood pressure and microalbuminuria in patients > or =65 years of age. METHODS: Of the 570 hypertensive patients with type 2 diabetes and persistent microalbuminuria in the NESTOR study, 187 (33%) individuals > or =65 years of age were included in this analysis. Of these, 95 patients received indapamide SR 1.5 mg and 92 patients received enalapril 10 mg, taken once daily in both cases. Adjunctive amlodipine and/or atenolol was added if required. RESULTS: The urinary albumin-to-creatinine ratio decreased by 46% in the indapamide SR group and 47% in the enalapril group. Noninferiority of indapamide SR over enalapril was demonstrated (P = .0236; 35% limit of noninferiority) with a ratio of 0.95 (95% CI: 0.68, 1.34). Mean arterial pressure decreased by 18 mm Hg and 15 mm Hg in the indapamide SR and the enalapril groups, respectively (P = .1136). The effects of both treatments seen in these elderly patients were similar to those observed in the main population, although the extent of the reduction in microalbuminuria was slightly higher. Both treatments were well tolerated, and no difference between groups was observed regarding glucose or lipid profiles. CONCLUSION: Indapamide SR is not less effective than enalapril in reducing microalbuminuria and blood pressure in patients aged >65 years of age with type 2 diabetes and hypertension.     

Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT1A activity, part 1

A series of new derivatives of 4-aryl-pyrido[1,2-c]pyrimidine containing the 3-(4-piperidyl)-1H-indole residue or its 5-methoxy derivative were synthesized. They were characterized (i) in vitro by binding to 5-HT(1A) receptors and 5-HT transporter proteins in rat brain cortex membranes and (ii) in vivo in the mouse by induced hypothermia and forced swimming models for antagonist/agonist activity against the 5-HT(1A) autoreceptors and postsynaptic 5-HT(1A) receptors, respectively. Structure activity relationship evaluation indicated that the presence of the 3-(4-piperidyl)-1H-indole residue and ortho- or para-substituents with -F or -CH(3) groups in the aryl ring as well as an unsubstituted aryl in the 4-aryl-pyrido[1,2-c]pyrimidine moiety promoted low K(i) values for both receptors. In contrast, the presence of a 5-methoxy-3-(4-piperidyl)-1H-indole residue as well as -Cl or -OCH(3) substituents at the para position markedly reduced the receptor affinity.     

Synthesis and biological investigation of potential atypical antipsychotics with a tropane core. Part 1

The synthesis, structure, in vitro and in vivo pharmacological activities of 3β-acylamine derivatives of tropane (4a-n, 5a-g, 6a,b, 8a-c) are described. Among the investigated compounds, several displayed very high (in nM) affinity for the monoamine receptors 5-HT(1A), 5-HT(2A,) and D(2). The most interesting agent 6b revealed very high affinity for the 5-HT(2A) and D(2) receptors and high affinity for the 5-HT(1A) receptor. The in vivo head twitch model was used to demonstrate antagonism of the 5-HT(2A) receptor subtype by this compound. In another test, 6b caused hypothermia in mice, which was not attenuated by WAY 100635. In the climbing test, the compound did not significantly modify climbing behaviour following apomorphine administration. Moreover, 6b significantly reduced locomotor activity in mice. Molecular docking studies using a homology model of the 5-HT(1A) receptor revealed a significant role of the N-8 atom of the tropane core in stabilising the ligand-receptor complex due to strong hydrogen bonding with Asp116 located in the TMH 3 helix. Analogically, in a homology model of the 5-HT(2A) receptor, the N-8 atom formed a hydrogen bond with Gly369. In another homology model of the D(2) receptor, strong hydrogen bonding of the amide moiety in the 3β position of the tropane nucleus with Asp85 was observed. Compound 6b displayed a favourable Meltzer index (1.21) which is a feature of atypical antipsychotic agents.     

Focus from superior vena cava and atypical atrioventricular nodal reentrant tachycardia in patient with paroxysmal atrial fibrillation--selective RF ablation

We describe a case of a 34-year-old woman with atrial fibrillation induced by focal frequent tachycardias from superior vena cava and atypical atrioventricular nodal reentrant tachycardia. Selective isolation of SVC and slow pathway RF ablation cured all types of atrial arrhythmias. The slow pathway was localised in the postero-septal mitral anulus and ablated from the left atrium.