Therapeutic Potential of Highly Selective A3 Adenosine Receptor Ligands in the Central and Peripheral Nervous System

Ligands of the G_i protein-coupled adenosine A₃ receptor (A₃R) are receiving increasing interest as attractive therapeutic tools for the treatment of a number of pathological conditions of the central and peripheral nervous systems (CNS and PNS, respectively). Their safe pharmacological profiles emerging from clinical trials on different pathologies (e.g., rheumatoid arthritis, psoriasis and fatty liver diseases) confer a realistic translational potential to these compounds, thus encouraging the investigation of highly selective agonists and antagonists of A₃R. The present review summarizes information on the effect of latest-generation A₃R ligands, not yet available in commerce, obtained by using different in vitro and in vivo models of various PNS- or CNS-related disorders. This review places particular focus on brain ischemia insults and colitis, where the prototypical A₃R agonist, Cl-IB-MECA, and antagonist, MRS1523, have been used in research studies as reference compounds to explore the effects of latest-generation ligands on this receptor. The advantages and weaknesses of these compounds in terms of therapeutic potential are discussed.     

Synthesis of novel azanorbornylpurine derivatives

Azanorbornylpurine derivatives were prepared by Mitsunobu reaction of appropriate hydroxyazanorbornane derivative with 6-chloropurine or construction of purine base at azanorbornylamines. The prepared target compounds were evaluated for antiviral activity and effect on neuronal and muscle nicotinic acetylcholine receptors.     

A Poset Fiber Theorem for Doubly Cohen-Macaulay Posets and Its Applications

This paper studies topological properties of the lattices of non-crossing partitions of types A and B and of the poset of injective words. Specifically, it is shown that after the removal of the bottom and top elements (if existent) these posets are doubly Cohen-Macaulay. This strengthens the well-known facts that these posets are Cohen-Macaulay. Our results rely on a new poset fiber theorem which turns out to be a useful tool to prove double (homotopy) Cohen- Macaulayness of a poset. Applications to complexes of injective words are also included.     

Magnetic fluid poly(ethylene glycol) with moderate anticancer activity

Poly(ethylene glycol) (PEG)-containing magnetic fluids - magnetite (Fe₃O₄) stabilized by sodium oleate - were prepared. Magnetic measurements confirmed superparamagnetic behaviour at room temperature. The structure of that kind of magnetic fluid was characterized using different techniques, including electron microscopy, photon cross correlation spectroscopy and small-angle neutron scattering, while the adsorption of PEG on magnetic particles was analyzed by differential scanning calorimetry and Fourier transform infrared spectroscopy. From the in vitro toxicity tests it was found that a magnetic fluid containing PEG (MFPEG) partially inhibited the growth of cancerous B16 cells at the highest tested dose (2.1 mg/ml of Fe₃O₄ in MFPEG).     

Solar Thermal Energy Storage in a Photochromic Macrocycle

The conversion and efficient storage of solar energy is recognized to hold significant potential with regard to future energy solutions. Molecular solar thermal batteries based on photochromic systems exemplify one possible technology able to harness and apply this potential. Herein is described the synthesis of a macrocycle based on a dimer of the dihydroazulene/vinylheptafulvene (DHA/VHF) photo/thermal couple. By taking advantage of conformational strain, this DHA–DHA macrocycle presents an improved ability to absorb and store incident light energy in chemical bonds (VHF–VHF). A stepwise energy release over two sequential ring‐closing reactions (VHF→DHA) combines the advantages of an initially fast discharge, hypothetically addressing immediate energy consumption needs, followed by a slow process for consistent, long‐term use. This exemplifies another step forward in the molecular engineering and design of functional organic materials towards solar thermal energy storage and release.     

Use of 9-methylfluorene as an indicator in the titration of common group IA and group IIA organometallic reagents

9-Methylfluorene was tested as an indicator in the titration of commonly used organometallic reagents. This indicator is readily prepared in three steps from fluorenone. In THF solution the deprotonated indicator is red and exhibits a sharp endpoint. The highly basic reagents sec-butyllithium and tert-butyllithium can be titrated in ether solution, where the color of the deprotonated indicator is yellow.     

Adhesion hysteresis in dynamic atomic force microscopy

The effects of adhesion hysteresis in the dynamic‐dissipation curves measured in amplitude‐modulation atomic force microscopy are discussed. Hysteresis in the interaction forces is shown to modify the dynamics of the cantilever leading to different power dissipation curves in the repulsive and attractive regimes. Experimental results together with numerical simulations show that power dissipation, as measured in force microscopy, is not always proportional to the energy dissipated in the tip–sample interaction process. (© 2008 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinheim)     

Über Nahordnung und elastisches Verhalten amorpher Hochpolymerer

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