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31.
32.
Mayumi Nishikata Aki Nakai Hitomi Fushida Keishiro Miyake Takaichi Arita Ken Iseki Katsumi Miyazaki Akikazu Nomura 《Journal of chromatography. B, Analytical technologies in the biomedical and life sciences》1993,612(2)
A method is described for the simultaneous determination of (+)- and (−)-homochlorcyclizine (HCZ) in human urine by high-performance liquid chromatography on a chiral stationary phase of ovomucoid-bonded silica. The pH of the buffer and organic modifier in the mobile phase markedly affected the chromatographic separation. A mobile phase of methanol—0.02 M acetate buffer (pH 4.7) (25:75, v/v) at a flow-rate of 1.0 ml/min was used for the urine assays. The ultraviolet absorption was monitored at 240 nm, and diphenhydramine was employed as the internal standard for the quantitation. (+)-HCZ, (−)-HCZ and the internal standard were eluted at retention times of 15, 25 and 8 min, respectively. The limit of determination for HCZ enantiomers was ca. 50 ng/ml of urine. One of the metabolites in human urine, which was a quaternary ammonium-linked glucuronide, could also be determined in a manner similar to unchanged HCZ after β-glucuronidase hydrolysis. A pharmacokinetic study was conducted with three healthy volunteers, who each received a single oral dose of racemic HCZ (20 mg). Distinct differences were found between the two enantiomers, particularly in the metabolic process, that is, the urinary excretion as (−)-HCZ-glucuronide within 48 h was ca. four times higher than that of the (+)-isomer. This method should be very useful for enantioselective pharmacokinetic studies of HCZ. 相似文献
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34.
Rhodopsinlike opsins constitute a distinct phylogenetic group (Yokoyama 1994, Mol. Biol. Evol. 11:32–39). This RH2 group includes the green-sensitive opsins in chicken and goldfish and the blue-sensitive opsin in a nocturnal lizard gecko. In the present study, we isolated and sequenced the genomic DNA clones for the RH2 opsin gene, rh2
Ac
, of the diurnal lizard Anolis carolinensis. This single-copy gene spans 18.3 kb from start to stop codons, making it the longest opsin gene known in vertebrates. Phylogenetic analysis strongly suggests that rh2
Ac
is more closely related to the chicken green opsin gene than to the gecko blue opsin gene. This gene tree differs from the organismal tree, where the two lizard species should be most closely related, implying that rh2
Ac
and the gecko blue-sensitive opsin genes have been derived from duplicate ancestral genes.Correspondence to: S. Yukiyama 相似文献
35.
Akira Uchimura Toshiyuki Shimizu Masahiro Morita Hitomi Ueno Kazuhiro Motoki Hideaki Fukushima Takenori Natori Yasuhiko Koezuka 《Bioorganic & medicinal chemistry》1997,5(12):2245-2249
We compared the immunostimulatory effects of chemically synthesized α-galactosylceramides (α-GalCers), α-glucosylceramides (α-GluCers), 6″-monoglycosylated α-GalCer and 6″- or 4″-monoglycosylated α-GluCer and made the following observations: (1) the length of the fatty acid side chain in the ceramide portions greatly affects the immunostimulatory effects of α-GalCers and α-GluCers; (2) the configuration of the 4″-hydroxyl group of the inner pyranose moiety plays an important role in the immunostimulatory effects of monoglycosylated α-
-pyranosylceramides; (3) the free 4″-hydroxyl group of the inner pyranose of monoglycosylated α-
-pyranosylceramides plays a more important role in their immunostimulatory effects than the free 6″-hydroxyl group. 相似文献
36.
Rika Morishita Shinsuke Saga Noriko Kawamura †Yoshio Hashizume ‡Toshiaki Inagaki Kanefusa Kato Tomiko Asano 《Journal of neurochemistry》1997,68(2):820-827
Abstract: The localization of two forms of the γ subunit of G proteins, γ3 and γ12, was examined in the mammalian brain. Concentrations of these two γ subunits increased markedly, as did those of glial fibrillary acidic protein, during postnatal development in the rat cerebral cortex. In aged human brains, by contrast, the concentration of γ3 tended to decrease with age, whereas that of γ12 in the temporal cortex increased slightly. An immunohistochemical study of human brains revealed that γ3 was abundant in the neuropil, whereas γ12 was localized in glial cells. In the hippocampal formation of aged human brains, levels of γ12-positive cells, as well as levels of glial fibrillary acidic protein- and vimentin-positive astrocytes, increased, in particular in the CA1 subfield and the prosubiculum, in which there was a decrease in the number of pyramidal cells. The appearance of γ12-positive cells associated with the loss of pyramidal cells was also observed in the hippocampus of rats that had been treated with kainic acid. These results indicate that γ12 is strongly expressed in reactive astrocytes. In a study of cultured neural cells, we found that γ12 was predominant in glioma cells, such as C6 and GA-1 cells, in contrast with the specific localization of γ3 in PC12 pheochromocytoma cells, which are neuron-like cells. Taken together, the results indicate that γ3 and γ12 are selectively expressed in neuronal and glial cells, respectively, and that concentrations of γ3 and γ12 in the brain are related to the numbers and/or extent of maturation of these cells. 相似文献
37.
38.
Prostaglandin D2 strongly inhibited growth of cultured mastocytoma P-815, 2-E-6 cells, which were established and cloned from mouse mast tumor cells. The inhibition was dose-dependent (IC50 = 2.09 × 10−5 M). Prostaglandin D2 also inhibited the DNA synthesizing activity of the cells dose-dependently. We next measured the activities of endogenous DNA polymerases extracted from untreated and prostaglandin D2-treated cells. Prostaglandin D2 pretreatment reduced DNA polymerase α activity by 52%. The sedimentation coefficients of the enzymes from untreated and prostaglandin D2-treated cells were the same suggesting there was no gross change in the size of the enzyme. Prostaglandin D2 pretreatment of the cells reduced endogenous DNA polymerase β activity to 68% of the control value; the sedimentation coefficients of the enzymes from treated and untreated cells were both 3.5 S. Interestingly, prostaglandin D2 had no direct inhibitory effect on the activity of either DNA polymerase α or β. Our results indicate that the activities of DNA polymerase α and β are lower in prostaglandin D2-treated mastocytoma cells. This finding account for the lower level of DNA synthesis in these cells. 相似文献
39.
The initial growth process of myelin figures, rod-like lyotropic liquid-crystalline structures, formed by phosphatidylcholine in water, ethylene glycol or glycerin, is suggested to be diffusion-limited with an apparent diffusion coefficient D of approx. 10(-6) cm2/s. D can be expressed by the sum of two processes. One is considered to describe the diffusion of an aggregate of phosphatidylcholine molecules and the other mainly to describe a lateral diffusion in the bilayer membranes which constitute myelin figures. 相似文献
40.
K Matsuyama K Moriwaki S Iida Y Itoh M Gomi S Kawamura S Tarui 《Endocrinologia japonica》1984,31(4):443-449
An extract of porcine thyroid gland in 0.1 N acetic acid exerted dose-dependent potentiation of ACTH-induced corticosterone production in isolated rat adrenal cells. The extract by itself manifested no steroidogenic activity. Upon gel-filtration of the extract, potentiating activities were demonstrated in three main peaks with molecular weights of about 10,000, 5,000 and 2,000. These findings indicate the presence of heterogeneous forms of ACTH-potentiating factors in the thyroid. Significant enhancement of ACTH-induced steroidogenesis was readily apparent with three gel-filtration fractions at a lower concentration of ACTH (4.75 pM). At this concentration, dose-dependent potentiation was observed with these three fractions. Enhanced corticosterone production responses by cells preincubated with the thyroid extract were observed and the results indicated the existence of potentiating mechanisms other than inhibition of ACTH proteolysis. The lack of T4, T3 and thyroglobulin in this activity suggests that the activity resides in other constituents of the thyroid. 相似文献