Discovery of an orally-active nonsteroidal androgen receptor pure antagonist and the structure-activity relationships of its derivatives

The 3-(4-cyano-3-trifluoromethylphenyl)-5,5-dimethylthiohydantoin derivatives which have carboxy-terminal side chains were synthesized and their agonistic/antagonistic activities against androgen receptor (AR) measured. Among them, compound 13b showed antagonistic activity (IC50=130 nM) with no agonistic activity even at 10000 nM. This compound exhibited significant metabolic stability and oral antiandrogenic activity (ED50=7 mg/kg).     

Tau neutrinos favored over sterile neutrinos in atmospheric muon neutrino oscillations

The previously published atmospheric neutrino data did not distinguish whether muon neutrinos were oscillating into tau neutrinos or sterile neutrinos, as both hypotheses fit the data. Using data recorded in 1100 live days of the Super-Kamiokande detector, we use three complementary data samples to study the difference in zenith angle distribution due to neutral currents and matter effects. We find no evidence favoring sterile neutrinos, and reject the hypothesis at the 99% confidence level. On the other hand, we find that oscillation between muon and tau neutrinos suffices to explain all the results in hand.     

Evaluation and applications of a new dye affinity adsorbent

The basic properties of a new dye affinity adsorbent Toyopearl AF-Blue HC-650M and its applications to the purification of proteins were studied. The binding capacity for human serum albumin (HSA) was greater than 18 mg per ml gel. The dye leakage from Toyopearl AF-Blue HC-650M in 0.5 M NaOH and 0.5 M HCI was less compared with an agarose adsorbent. Caustic stability study also demonstrated this material withstood exposure to 0.1 M NaOH for 1 month with no significant loss of binding capacity for HSA. We purified human albumin from human serum and lactate dehydrogenase (LDH) from rabbit muscle extract in a single step. Sodium dodecylsulfate-polyacrylamide gel electrophoresis indicates that human albumin and LDH were highly purified.     

Fiber-optic sensor for carbon dioxide with a ph indicator dispersed in a poly(ethylene glycol) membrane

A fiber-optic sensor for carbon dioxide gas is constructed, without an inner buffer solution, by using a dispersion of fluorescein in poly(ethylene glycol) deposited on the distal end of an optical fiber. Evaporation of the solvent is thus negligible. The response range is 0–28% (v/v) for carbon dioxide, with a detection limit of 0.1%. The response time achieved is 10 s. The membrane (ca. 10 μm thick) is composed of poly(ethylene glycol)s with molecular weights of 200 and 1540 dalton in a 20:80% (w/w) ratio. The best concentration of fluorescein is 5 × 10^?7 mol g^?1 of poly(ethylene glycol). The response mechanism of the sensor is discussed.     

Measurement of the fragmentation of Carbon nuclei used in hadron-therapy

The increasing use of Carbon nuclei in cancer therapy centres is motivated by their potential advantages as a very precise high LET radiation. The knowledge of the fragmentation of Carbon nuclei when they interact with the human body is important to evaluate the spatial profile of their energy deposition in the tissues, hence the damage to the tissues neighbouring the tumour. We report here a study of the fragmentation with the nuclear emulsion experimental technique. We have designed, built and exposed to a Carbon nuclei beam a chamber made of Lexan plates alternated with nuclear emulsion films. Lexan plates acted as passive material simulating human body tissues while nuclear emulsion films were used as both tracking devices with micrometric accuracy and ionisation detectors. Such a detector allowed the detection of Carbon interactions produced along their path, the identification of the fragments produced and the measurement of their scattering angle. We have measured the Carbon ion survival probability and studied their interactions. We report on the secondary particle multiplicity and the electrical charge distribution. We give results of the scattering angle of final state fragments as well as the range for H and He. Finally we give the total and partial charge-changing cross-sections for Δz=1,2,3,4$\mathrm{\Delta }z=1,2,3,4$ which are compared with previous results when available. The present work aims at providing data required as input to Monte Carlo simulations of Carbon ion interactions in the human body and ultimately of their therapeutic effectiveness.