Synthesis and Preliminary Evaluation of 11C-Labeled VU0467485/AZ13713945 and Its Analogues for Imaging Muscarinic Acetylcholine Receptor Subtype 4

Muscarinic acetylcholine receptors (mAChRs) have five distinct subunits (M₁–M₅) and are involved in the action of the neurotransmitter acetylcholine in the central and peripheral nervous system. Attributed to the promising clinical efficacy of xanomeline, an M₁/M₄-preferring agonist, in patients of schizophrenia and Alzheimer's disease, M₁- or M₄-selective mAChR modulators have been developed that target the topographically distinct allosteric sites. Herein we report the synthesis and preliminary evaluation of ¹¹C-labeled positron emission tomography (PET) ligands based on a validated M₄R positive allosteric modulator VU0467485 (AZ13713945) to facilitate drug discovery. [¹¹C]VU0467485 and two other ligands were prepared in high radiochemical yields (>30 %, decay-corrected) with high radiochemical purity (>99 %) and high molar activity (>74 GBq μmol⁻¹). In vitro autoradiography studies indicated that these three ligands possess moderate-to-high in vitro specific binding to M₄R. Nevertheless, further physiochemical property optimization is necessary to overcome the challenges associated with limited brain permeability.     

Compact electrostatic levitator for diffraction measurements with a two axis diffractometer and a laboratory x-ray source

A compact electrostatic levitator was developed for the structural analysis of high-temperature liquids by x-ray diffraction methods. The size of the levitator was 200 mm in diameter and 200 mm in height and can be set up on a two axis diffractometer with a laboratory x-ray source, which is very convenient in performing structural measurements of high-temperature liquids. In particular, since the laboratory x-ray source allows a great amount of user time, preliminary or challenging experiments can be performed with trial and error, which prepares and complements synchrotron x-ray experiments. The present small apparatus also provides the advantage of portability and facility of setting. To demonstrate the capability of this electrostatic levitator, the static structure factors of alumina and silicon samples in their liquid phases were successfully measured.     

Preparation of poly(thiophene-alt-pyrrole) bearing chiral LC group

ABSTRACT

Preparation of poly(thiophene-alt-pyrrole bearing mesogen) was carried out with Migita–Kosugi–Stille coupling type polycondensation with an aid of Pd(0) complex catalyst. The resultant polymer shows lyotropic liquid crystallinity with good film-forming property. The smectic fan-shaped texture is maintained after completion of evaporation of solvent from the polymer solution. The cast film having liquid crystal (LC) order shows light emission function upon irradiation of excitation light at 460 nm. The polymer shows LC domain emission. Mechanical orientation allows to yield LC domain aligned film with band structure. Chiral mesogenic side chain induces π-conjugated main chain helicity from distance in molecular level.     

Preparation of Cu2ZnSnS4 thin films by sulfurizing electroplated precursors

Cu₂ZnSnS₄ (CZTS) thin films were prepared by sulfurizing precursors deposited by electroplating. The precursors (Cu/Sn/Zn stacked layers) were deposited by electroplating sequentially onto Mo-coated glass substrates. Aqueous solutions containing copper sulfate for Cu plating, tin sulfate for Sn plating and zinc sulfate for Zn plating were used as the electrolytes. The precursors were sulfurized by annealing with sulfur at temperatures of 300, 400, 500 and 600 °C in an N₂ gas atmosphere. The X-ray diffraction peaks attributable to CZTS were detected in thin films sulfurized at temperatures above 400 °C. A photovoltaic cell using a CZTS thin film produced by sulfurizing an electroplated Sn-rich precursor at 600 °C exhibited an open-circuit voltage of 262 mV, a short-circuit current of 9.85 mA/cm² and an efficiency of 0.98%.     

Polymerization of β-lactoglobulin and bovine serum albumin at oil-water interfaces in emulsions by transglutaminase

Polymerization of β-lactoglobulin and bovine serum albumin at the oil—water interfaces in n-tetradecane-in-water emulsions induced by the transglutaminase reaction was studied. The emulsions were incubated with transglutaminase for various times, and adsorbed and unadsorbed protein fractions at the oil—water interfaces were analyzed by sodium dodecyl sulfate—polyacrylamide gel electrophoresis. While only monomers were detected in the unadsorbed fractions, polymers were observed in the adsorbed fractions of the both proteins. The sizes and amounts of the polymers increased with incubation time. The incubation with transglutaminase caused much flocculation of the emulsion stabilized by β-lactoglobulin. An increase in viscosity was also observed with the flocculation. The flocculation was probably initiated by the formation of ε-(γ-glutamyl)-lysyl isopeptide bonds between β-lactoglobulin molecules adsorbed on different oil droplets. In the case of the emulsion stabilized by bovine serum albumin, however, the flocculation and the increase in viscosity occurred to only limited extents by the transglutaminase reaction. This suggests that ε-(γ-glutamyl)-lysyl isopeptide bonds induced by the transglutaminase reaction were formed only between neighboring molecules of bovine serum albumin on the same droplet.     

Fluctuations in the cerebral oxygenation state during the resting period in functional mapping studies of the human brain

Functional mapping studies using near-infrared spectroscopy have detected for the first time the existence of significant fluctuations in the concentration of cerebral oxygenated [oxy-Hb], and deoxygenated haemoglobin, [deoxy-Hb], during the resting period. The fluctuations are not related to alterations in the systemic circulatory system. The temporal pattern varies with each brain region. In some instances, the degrees of change in [oxy-Hb] and [deoxy-Hb] caused by highly integrated tasks are within this resting variation range. Thus, taking account of these fluctuations is essential to the interpretation of distribution patterns of cerebral activity.     

A Small-Corpus-Based Approach to Alice's Roles

This paper is a case study for examining how a small-corpus-basedapproach can contribute to research in stylistics. Specifically,we have built small corpora of the two Alice books and retrieved,using WordSmith Tools suite, first, verbs of saying and theiradverbials to elucidate how Alice speaks to others in the stories,and secondly, modifiers of ‘Alice’ to get the imagesof the main character. An analysis of these data reveals thatAlice's role in each book is quite distinct: an unexpected visitorthrown into the passive state in Wonderland and an active explorerin Looking-Glass. These findings objectively serve to reinforceour argument over what Alice is called through the perusal ofthe texts. Alice's roles in the two books are thus interactivelysupported by the small-corpus-based approach and the non-corpus-basedapproach, which may explore the validity of the interfaced approach,the collaborative work of quantitative processing and qualitativespeculation.     

A Study on the Distances of Small Mobile Robot Moves towards Infants

In recent years, it is remarkable that various robots are being developed, and the development of robot technology is beginning to be taken into an actual living space. There are still many questions that we will have to answer for the harmonization of living together with a robot. This study is focused on ＂the study of how to plan and design a living space in harmonizing with robots＂, and focused on the effects of infants （subjects） along with the distance between robots and themselves. The study is to seek for the minimum distance for the subjects who felt that ＂I do not want a robot to be any closer being approached to me＂. This experiment was conducted among 30 infants at the kindergarten, utilizing a small experimental robot. A small robot whose dimension is 120 mm （W） ×130 mm （D） × 70 mm （H）, approaching infants as is to see if it would make any differences to the infant＇s reactions.     

Study on Heat Transfer and Flow Characteristic Under Phase-Change Process of an Acoustically Levitated Droplet

Acoustic levitation is one of the levitation technique which is expected to be used for analytical chemistry and manufacturing new materials. Thus, it is important to gather the knowledge about acoustically levitated droplet. The purpose of this study is to investigate the heat transfer and flow behavior under phase change process of an acoustically levitated droplet. The following results were obtained from experiments. Evaporation process and external flow structure of the levitated droplet is visualized by a high speed camera and it is found that they differ by the type of fluid. Toroidal vortices are observed near the surface of the ethanol solution droplet. Heat transfer coefficient is estimated from the volume change and temperature gradient. It is substantially higher than that estimated by the existing experimental correlation.