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1.
Cerebellar granule cells (CGNs) are one of many neurons that express phasic and tonic GABAergic conductances. Although it is well established that Golgi cells (GoCs) mediate phasic GABAergic currents in CGNs, their role in mediating tonic currents in CGNs (CGN-Itonic) is controversial. Earlier studies suggested that GoCs mediate a component of CGN-Itonic that is present only in preparations from immature rodents. However, more recent studies have detected a GoC-dependent component of CGN-Itonic in preparations of mature rodents. In addition, acute exposure to ethanol was shown to potentiate the GoC component of CGN-Itonic and to induce a parallel increase in spontaneous inhibitory postsynaptic current frequency at CGNs. Here, we tested the hypothesis that these effects of ethanol on GABAergic transmission in CGNs are mediated by inhibition of the Na+/K+-ATPase. We used whole-cell patch-clamp electrophysiology techniques in cerebellar slices of male rats (postnatal day 23–30). Under these conditions, we reliably detected a GoC-dependent component of CGN-Itonic that could be blocked with tetrodotoxin. Further analysis revealed a positive correlation between basal sIPSC frequency and the magnitude of the GoC-dependent component of CGN-Itonic. Inhibition of the Na+/K+-ATPase with a submaximal concentration of ouabain partially mimicked the ethanol-induced potentiation of both phasic and tonic GABAergic currents in CGNs. Modeling studies suggest that selective inhibition of the Na+/K+-ATPase in GoCs can, in part, explain these effects of ethanol. These findings establish a novel mechanism of action of ethanol on GABAergic transmission in the central nervous system. 相似文献
2.
H Miyazaki T Fujii H Amejima N Mikuriya K Nambu A Kagemoto M Nakao Y Oh-e K Matsumoto Y Matsui 《Biotherapy》1988,1(1):7-18
Disposition of [125I]rHu-TNF was elucidated in BALB/c mice bearing Meth A fibrosarcoma 7 days after transplantation. After i.v. administration, [125I]rHu-TNF measured by radioactivity and immunoreactivity biphasically decreased in plasma. Tumor level of [125I]rHu-TNF was the maximum at 1 h, then decreased and finally remained essentially constant. After i.t. administration, plasma level reached the maximum at 1 h. Tumor level decreased quickly and then became essentially constant. [125I]rHu-TNF was suggested to be degraded to small fragments in the tumor. Significant distribution of [125I]rHu-TNF was found in the kidney, lung, liver and tumor. Most tissue levels decreased with time in parallel with plasma levels. [125I]rHu-TNF radioactivity was found in proximal convoluted tubules of kidney and in those areas of tumor consisting of degenerating cells with pyknotic nuclei. Urine contained most of administered radioactivity, which being neither immunoreactive nor protein-bound. 相似文献
3.
4.
Hisashi Miyazaki Masatoshi Iida Yoshimasa Matsunaga Toshihiko Fujii Keiko Nambu Hideki Amejima Yoshinori Oh-e Hideo Furukawa Yukiharu Matsui Yasunobu Sohmura Masahisa Hashimoto 《Biotherapy》1989,1(1-2):47-57
The mode of antitumor action of rHu-TNF was elucidated in BALB/c mice bearing Meth A fibrosarcoma 7 days after transplantation with respect to time course, dose-response relationships and selectivity of the effects. The maximal cytotoxic effect on tumor cells revealed by inhibition of DNA synthesis and maximal lesional effect on tumor vasculature revealed by change in blood pool-size in the tissue were detected at 30 min and I h after administration of rHu-TNF, respectively. The dose-response relationship between cytotoxic and tumoricidal effects of rHu-TNF was irrespective of administration route. ED50s of these antitumor effects afteri.v. administration of rHu-TNF were about 50 times as high as ED50s afteri.t. administration. ED50 ofi.t. given rHu-TNF for vascular effect was about 20 times as high as that for cytotoxicity while ED50 ofi.v. rHu-TNF for vascular effect was only 2–3 times as high as that for cytotoxicity. The whole body autoradiographies with [125I] HSA giveni.v. to see the blood influx into tumor tissue and [14C]thymidine given i.v. to see DNA synthesis in the whole body after administration of rHu-TNF revealed that the distribution of radioactivity was markedly changed in the tumor alone without any detectable change in other whole body tissues.In conclusion, thein vivo antitumor effect of rHu-TNF giveni.t. ori.v., appears to be exerted through the direct action on Meth A sarcoma rather than indirectly on tumor vasculature. Under present conditions, the effect of rHu-TNF in the whole body tissues seems rather selective on cells and vasculature of the tumor. 相似文献
5.
Dr. Sherif M. H. Sanad Alshimaa A. M. Abdelsalam Aya A. Gamal Eldin Esraa H. Abdelfattah Fatma R. M. Hussein Nada G. Mohammed Nariman A. S. Taha Prof. Dr. Ahmed E. M. Mekky 《化学与生物多样性》2023,20(6):e202300546
An efficient protocol was adopted to efficiently prepare three new series of bis(pyrazolo[1,5-a]pyrimidines) linked to different spacers. The new bis(pyrazolo[1,5-a]pyrimidines) were prepared in 80–90 % yields by reacting the respective bis(enaminones) and 4-(4-substituted benzyl)-1H-pyrazole-3,5-diamines in pyridine at reflux temperature for 5–7 h. The new products showed a wide spectrum of antibacterial activity against six different bacterial strains. In general, propane- and butane-linked bis(pyrazolo[1,5-a]pyrimidines), which are attached to 3-(4-methyl- or 4-methoxybenzyl) units, had the best antibacterial activity with minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values up to 2.5 and 5.1 μM, respectively. Additionally, the previous products demonstrated promising MurB inhibitory activity with IC50 values up to 7.2 μM. 相似文献
6.
Pierluigi Gariboldi Francesca Pelizzoni Marco Tat Luisella Verotta Nadia El-Sebakhy Aya M. Asaad Rokia M. Abdallah Soad M. Toaima 《Phytochemistry》1995,40(6):1755-1760
Three new cycloartane glycosides, trigonoside I, II and III, and the known astragalosides I and II were isolated from the roots of Astragalus trigonus. The structures of the new glycosides were totally elucidated by high field (600 MHz) NMR analyses as cycloastragenol-6-O-β-xylopyranoside, cycloastragenol-3-O-[-l-arabinopyranosyl(1 → 2)-β-d-xylopyranosyl]-6-O-β- d-xylopyranoside and cycloastragenol-3-O-[-l-arabinopyranosyl(1 → 2)-β-d-(3-O-acetyl)-xylopyranosyl]-6-O-β-d-xylopyranoside. 相似文献
7.
When everted sacs of rat duodenum, jejunum and ileum were incubated with [14C]loperamide in vitro, unchanged drug and its metabolites were found not only in tissues but also in media of the mucosal side with virtually no radioactivity in media of the serosal side. The amounts of metabolites found in media of the mucosal side were comparable to or larger than those in tissues. Di-desmethyl loperamide was more predominant in the media as compared with mono-demethylated one than in the tissues. Therefore, a portion of loperamide absorbed in intestines can be metabolized there and directly secreted back into lumen. Oral loperamide thus undergoes a unique disposition, likely constituting one of mechanisms for its distinct dissociation of central and antidiarrheal activities. 相似文献
8.
The relationship between the binding patterns of soybean agglutinin, peanut agglutinin (both in their native (unaggregated) form and in their polymerized form), and of Phaseolus vulgaris leucoagglutinin, to neuraminidase-treated lymphocytes from different sources, and the mitogenic activity of these lectins, was studied. In all cases investigated, binding of a lectin to lymphocytes which resulted in stimulation was a positive cooperative process. Our findings support the assumption that clustering of receptors and conformational changes in membrane structure are prerequisites for mitogenic stimulation. 相似文献
9.
Atushi Ushimaru Satoshi Kikuchi Ryuji Yonekura Atsushi Maruyama Nao Yanagisawa Maiko Kagami Michiko Nakagawa Suzuki Mahoro Yukihiko Kohmatsu Aya Hatada Shumpei Kitamura Kensuke Nakata 《Nordic Journal of Botany》2004,24(5):593-598
We compared the amount of variation in flower size between autogamous and insect-pollinated species to examine the hypothesis that pollinator-mediated selection stabilizes flower size in plant populations. One would expect the flower size variation to be larger in selfing species that are less affected by pollinator-mediated stabilizing selection than in insect-pollinated species. The results of phylogenetic comparisons between autogamous and insect-pollinated flowers supported the pollinator-mediated stabilizing selection hypothesis, although the non-phylogenetic comparison did not. According to our results, we discuss the factors influencing the flower size variation. 相似文献
10.
Danielle M. Kirkpatrick Kevin B. Rice Aya Ibrahim William R. Morrison Tracy C. Leskey 《Entomologia Experimentalis et Applicata》2019,167(12):1020-1029
The brown marmorated stink bug, Halyomorpha halys (Stål) (Hemiptera: Pentatomidae), is a polyphagous invasive insect and currently one of the most threatening agricultural pests in the USA and globally. Nymphs are highly mobile, moving among host plants, and causing significant damage. Thus, understanding dispersal biology for all life stages is critical for the development of reliable monitoring and management programs. Here, we evaluated the influence of harmonic radar as a tool to study dispersal ecology of nymphal H. halys; we measured the impact of glues and tag attachment on survivorship and mobility in the laboratory and validated in the field that tagged and released nymphs could be tracked on baited and unbaited host and non‐host plants using harmonic radar. In the laboratory, four glues were evaluated for attaching harmonic radar tags securely to nymphs, and survivorship with attached tags was measured. There were no significant differences in survivorship or vertical and horizontal movement among nymphs with tags affixed with the glue treatments compared with the untagged control. Based on numerically greater survivorship of nymphs with tags affixed with Loctite glass glue, a field validation study of tagged nymphs released in host (apple tree) and non‐host (mowed grass) with or without H. halys pheromonal stimuli present revealed that nymphs could be successfully relocated using harmonic radar after 48 h. Among treatments, 83% of nymphs remained in baited and unbaited apple trees, 50% of nymphs remained in baited mowed grass plots, and in unbaited mowed grass plots, 17% of fifth instars, and 0% of fourth instars were retained. The absence of negative effects on mobility, survivorship, and field tracking validates that harmonic radar can be used to study dispersal ecology of nymphal H. halys. 相似文献