Metabolism of a new P-glycoprotein inhibitor HM-30181 in rats using liquid chromatography/electrospray mass spectrometry

HM-30181, 4-oxo-4H-chromene-2-carboxylic acid, [2-(2-{4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-ethyl]-phenyl}-2H-tetrazol-5-yl)-4,5-dimethoxyphenyl]amide, is a new P-glycoprotein inhibitor. This study was performed to identify the in vitro and in vivo metabolic pathway of HM-30181 in rats. Rat liver microsomal incubation of HM-30181 in the presence of NADPH resulted in the formation of four metabolites, M1-M4. M1 and M2 were identified as 2-(2-{4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-ethyl]-phenyl}-2H-tetrazol-5-yl)-4,5-dimethoxyaniline and 4- or 5-O-desmethyl-HM-30181, respectively, on the basis of liquid chromatography/tandem mass spectrometry (LC/MS/MS) analysis with the synthesized authentic standards. M3 and M4 were suggested to be 6- or 7-O-desmethyl-HM-30181 and hydroxy-HM-30181, respectively. These in vitro metabolites were also detected in feces and urine samples after an intravenous administration of HM-30181 to male rats. The metabolic routes for HM-30181 were O-demethylation of the methoxy group to M2 and M3, hydrolysis of the amide group to M1, and hydroxylation to M4.     

Versatile control of geometric birefringence in elliptical hollow optical fiber

A novel optical fiber fabrication technique was developed by converting the symmetry of the silica substrate into the germanosilicate ring core to efficiently introduce geometric birefringence in an elliptical hollow optical fiber. Due to high ellipticity in the hollow ring core, the fiber provides an extremely high group birefringence of 2.35 x 10(-3) at 1550 nm. Single-mode single-polarization guidance was also experimentally confirmed, with a bandwidth of approximately 35 nm. The generic adiabatic mode conversion capability in the taper also provided a stable fusion splice to conventional single-mode fiber with low loss and high tensile strength.     

Oligobisvelcraplex: self-assembled linear oligomer by solvophobic pi-pistacking interaction of bisvelcrands based on resorcin[4]arene

[reaction: see text] Bisvelcrand 3 based on resorcin[4]arene was obtained by a stepwise route, and the formation of oligobisvelcraplex 3(n) by solvophobic pi-pistacking interaction was observed. (1)H NMR spectroscopic studies revealed that DeltaG(++)(pseudorotation) of oligobisvelcraplex 3(n) is 16.7 kcal mol(-1) in C(6)D(5)NO(2) solution. The pulsed field gradient spin-echo (PGSE) NMR experiment and VPO experiment showed that the number of aggregation (n) ranges from 7 to 10 in CHCl(3) solution at 298 K. In high concentration, bisvelcrand 3 tends to form gels or fiber.     

High Differential Group Index of Dispersion Compensating Fibers for OCDMA Encoder/Decoder

We report the LPG pair device that can be used as a pulse duplicator or an OCDMA encoder/decoder. Due to the ring core region of dispersion compensating fiber (DCF), we can shorten the device length by a third and obtain surrounding insensitive LPG devices.     

Filter characteristics of a chirped volume holographic grating

We compare and analyze the filter properties of transmission-type volume holographic gratings, especially the dispersion characteristics for uniform and chirped gratings. It is theoretically and experimentally shown that the dispersion characteristics can be controlled by introducing one-dimensional chirping to the volume grating in a photorefractive crystal. The filter response including output power and dispersion comes from a combined effect of the spatial spectra of the grating structure, input beam, and output-coupling fiber mode. Filter responses can be designed by controlling these parameters for optical communication applications.     

A method for estimating the parameters of electrodynamic drivers in thermoacoustic coolers

The electroacoustic efficiency of high-power actuators used in thermoacoustic coolers may be estimated using a linear model involving a combination of six parameters. A method to identify these equivalent driver parameters from measured total electrical impedance and velocity-voltage transfer function data was developed. A commercially available, moving-magnet driver coupled to a functional thermoacoustic cooler was used to demonstrate the procedure experimentally. The method, based on linear electrical circuit theory, allowed for the possible frequency and amplitude dependence of the driver parameters to be estimated. The results demonstrated that driver parameters measured in vacuo using this method can be used to predict the driver efficiency and performance for operating conditions which may be encountered under load.     

Complete determination of the stress tensor of a polarization-maintaining fiber by photoelastic tomography

The use of photoelastic tomography to obtain the two-dimensional axial stress profile of a polarization-maintaining (PM) fiber with high resolution and accuracy is described. We illustrate, for what is believed to be the first time, the two-dimensional distribution of the local principal axes of the fiber's cross section, which is directly related to the fiber's PM ability. We demonstrate that the stress-induced anisotropy as well as all the stress tensor components of the fiber can be fully determined.     

Residual stress relaxation in the core of optical fiber by CO(2) laser irradiation

We observed residual stress relaxation by CO(2) laser irradiation in the cores of optical fibers by direct stress measurement. It was demonstrated that the mechanical stress was fully relaxed by CO(2) laser irradiation and that the remaining stress in the core was thermal stress that was due to a mismatch of the thermal expansion coefficients of the fiber core and cladding. The net core stresses after relaxation were 17, 68, and 203 MPa in Ge-B-codoped fibers drawn at 0.53, 1.38, and 3.48 N, respectively. Changes in the refractive indices of the cores as a result of residual stress relaxation were also estimated.     

Production of rapidly reversible antibody and its performance characterization as binder for continuous glucose monitoring

To effectively control diabetes, a method to reliably measure glucose fluctuations in the body over given time periods needs to be developed. Current glucose monitoring systems depend on the substrate decomposition by an enzyme to detect the product; however, the enzyme activity significantly decays over time, which complicates analysis. In this study, we investigated an alternative method of glucose analysis based on antigen-antibody binding, which may be active over an extended period of time. To produce monoclonal antibodies, mice were immunized with molecular weight (M(W)) 10K dextran chemically conjugated with keyhole limpet hemocyanin. Since dextran contains glucose molecules polymerized via a 1,6-linkage, the produced antibodies had a binding selectivity that could discriminate biological glucose compounds with a 1,4-linkage. Three antibody clones with different affinities were screened using the M(W) 1K dextran-bovine serum albumin conjugates as the capture ligand. Among the antibodies tested, the antibody clone Glu 26 had the lowest affinity (K(A) = 3.56 × 10(6) M(-1)) and the most rapid dissociation (k(d) = 1.17 × 10(-2) s(-1)) with the polysaccharide immobilized on the solid surfaces. When glucose was added to the medium, the sensor signal was inversely proportional to the glucose concentration in a range between 10 and 1000 mg dL(-1), which covered the clinical range. Under the optimal conditions, the response time was about 3 min for association and 8 min for dissociation based on a 95% recovery of the final equilibrium.