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排序方式: 共有134条查询结果,搜索用时 15 毫秒
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Frank P. Zemlan Anne Zieleniewski-Murphy R. Maureen Murphy Michael M. Behbehani 《Neurochemistry international》1990,16(4):515-522
Recent data indicate that BMY 7378 demonstrates high affinity, selectivity and low intrinsic activity at hippocampal 5-HT1A receptors, suggesting that BMY 7378 may represent the first selective 5-HT1A functional antagonist. The present study examined the agonist and antagonist properties of BMY 7378 at spinal cord 5-HT1A receptors. In electrophysiological studies, iontophoretic administration of either the 5-HT1A agonist 8-OH-DPAT (43.8 ± 5.4 nA) or BMY 7378 (46.3 ± 5.2 nA) significantly inhibited the firing rate of wide-dynamic-range dorsal horn units indicating that BMY 7378 demonstrates significant intrinsic activity at spinal cord 5-HT1A receptors. Concomitant BMY 7378 and 8-OH-DPAT administration identified no BMY 7378 ejection current (20–100 nA) which antagonized the 8-OH-DPAT induced inhibition of dorsal horn unit activity. In behavioral studies in the spinal rat, 8-OH-DPAT increased the animals' sensitivity to noxious levels of mechanical stimulation (ED50 = 269 ± 24 nmol/kg) as did BMY 7378 (ED50 = 295 ± 70 nmol/kg) with no statistically significant difference in the maximal response (Ymax) observed. Concomitant BMY 7378 and 8-OH-DPAT administration identified no BMY 7378 dose (10–1100 nmol/kg) which blocked the hyperalgesic effect of 8-OH-DPAT, rather, each drug produced similar effects which were additive. Further, the 5-HT1A agonist effects of BMY 7378 were blocked by the 5-HT1A antagonist, spiperone. Therefore, both the electrophysiologic and reflex data indicate that BMY 7378 possesses significant intrinsic activity at spinal cord 5-HT1A receptors, and like 8-OH-DPAT is a partial agonist at these receptors. Differences in BMY 7378 intrinsic activity at spinal cord as opposed to hippocampal 5-HT1A receptors are discussed in terms of regional differences in G-proteins coupled to 5-HT1A receptors in these two CNS regions. 相似文献
3.
The influence of GABA on cells in the gustatory region of the hamster solitary nucleus 总被引:2,自引:1,他引:1
A brainstem slice preparation was used to investigate GABA-inducedresponses in the gustatory region of the nucleus of the solitarytract (NST) of the hamster. The baseline activities of 91 cellsin the rostral NST were examined extracellularly; 59 cells werelocated in the rostral central (RC), 21 in the rostral lateral(RL), six in the ventral (V) and five in the medial (M) subdivisionof the NST. Of the 80 cells in the gustatory region of the NST(RC and RL subdivisions), application of GABA produced dose-dependentinhibition in 55 (69%), excitation in 9 (11%) and no effectin 16 cells (22%). In contrast, only nine cells were responsiveto baclofen, a GABAB agonist. In all subdivision of the rostralNST, 57 cells were inhibited by GABA and the responses of 48of these were blocked by the specific GABAA antagonist, bicucullinemethiodide (BICM). Application of BICM alone often yielded anexcitatory burst of impulses; this effect was eliminated whensynaptic release was blocked by perfusion with a high magnesiumphysiological saline solution (PSS/Mg++). The GABAA-responsivecells were distributed predominantly within the RC subdivision,whereas the GABAB-responsive neurons were mostly in the RL subdivisionof the NST. The influences of GABA on the membrane properties of cells withinthe gustatory region (RC and RL subdivisions) of the NST wererecorded using conventional intracellular (16 cells) or whole-cellpatch (17 cells) recording methods. Intracellular recordingrevealed that GABA produced hyperpolarisation of the membrane,decreased the firing frequency, and increased the membrane conductance.In the patch-clamp experiments, the application of GABA evokedboth inward and outward currents, and an increase in membraneconductance. The reversal potential produced by GABA was closeto the Cl equilibrium potential. The effects of GABAwere blocked by BICM. These results suggest that (i) GABA hasa strong inhibitory influence on rostral NST neurons, whichin the majority of cells is mediated through GABAA, receptors;and (ii) the gustatory region of the NST may contain a tonicallyactive GABAergic netw 相似文献
4.
A simple and convenient method for culturing anaerobic bacteria is described. Cultures can be grown in commercially available flasks normally used for preparation of sterile external solutions. A special disposable rubber flask closure maintains anaerobic conditions in the flask after autoclaving. Growth of a variety of anaerobic oral bacteria was comparable to that obtained after anaerobic incubation of broth cultures in Brewer Anaerobic Jars. 相似文献
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Almehdar Hussein A. El-Baky Nawal Abd Alhaider Abdulqader A. Almuhaideb Saud A. Alhaider Abdullah A. Albiheyri Raed S. Uversky Vladimir N. Redwan Elrashdy M. 《Probiotics and antimicrobial proteins》2020,12(1):18-31
Probiotics and Antimicrobial Proteins - Lactoferrin is an iron-binding glycoprotein present in various secretions (e.g., milk, tears, saliva, pancreatic juice), which performs multiple functions,... 相似文献
7.
Loai M. Alnemer Raed I. Seetan Filippo M. Bassi Charith Chitraranjan Adam Helsene Paul Loree Steve Bou Goshn Yong Q. Gu Ming-Cheng Luo M. Javed Iqbal Gerard R. Lazo Anne M. Denton Shahryar F. Kianian 《Functional & integrative genomics》2013,13(1):11-17
In the course of evolution, the genomes of grasses have maintained an observable degree of gene order conservation. The information available for already sequenced genomes can be used to predict the gene order of nonsequenced species by means of comparative colinearity studies. The “Wheat Zapper” application presented here performs on-demand colinearity analysis between wheat, rice, Sorghum, and Brachypodium in a simple, time efficient, and flexible manner. This application was specifically designed to provide plant scientists with a set of tools, comprising not only synteny inference, but also automated primer design, intron/exon boundaries prediction, visual representation using the graphic tool Circos 0.53, and the possibility of downloading FASTA sequences for downstream applications. Quality of the “Wheat Zapper” prediction was confirmed against the genome of maize, with good correlation (r?>?0.83) observed between the gene order predicted on the basis of synteny and their actual position on the genome. Further, the accuracy of “Wheat Zapper” was calculated at 0.65 considering the “Genome Zipper” application as the “gold” standard. The differences between these two tools are amply discussed, making the point that “Wheat Zapper” is an accurate and reliable on-demand tool that is sure to benefit the cereal scientific community. The Wheat Zapper is available at http://wge.ndsu.nodak.edu/wheatzapper/. 相似文献
8.
Al-Qawasmeh RA Lee Y Cao MY Gu X Vassilakos A Wright JA Young A 《Bioorganic & medicinal chemistry letters》2004,14(2):347-350
Clotrimazole (CLT) 1, a synthetic anti-fungal imidazole derivative, inhibits tumor cell proliferation and angiogenesis. In the current study, flow cytometric analysis demonstrated that the decrease in tumor cell growth by CLT 1 was associated with inhibition of cell cycle progression at the G(1)-S phase transition, resulting in G(0)-G(1) arrest. A series of CLT 1 analogues has been generated in order to develop CLT 1 derivatives that are devoid of the imidazole moiety which is responsible for the hepatoxicity associated with CLT 1 while retaining CLT 1 efficacy. The majority of these analogues demonstrate in vitro antiproliferative activity ranging from submicromolar to micromolar concentrations. 相似文献
9.
Zhang R Behbehani K Crandall CG Zuckerman JH Levine BD 《American journal of physiology. Heart and circulatory physiology》2001,280(1):H407-H419
To examine the dynamic properties of baroreflex function, we measured beat-to-beat changes in arterial blood pressure (ABP) and heart rate (HR) during acute hypotension induced by thigh cuff deflation in 10 healthy subjects under supine resting conditions and during progressive lower body negative pressure (LBNP). The quantitative, temporal relationship between ABP and HR was fitted by a second-order autoregressive (AR) model. The frequency response was evaluated by transfer function analysis. Results: HR changes during acute hypotension appear to be controlled by an ABP error signal between baseline and induced hypotension. The quantitative relationship between changes in ABP and HR is characterized by a second-order AR model with a pure time delay of 0.75 s containing low-pass filter properties. During LBNP, the change in HR/change in ABP during induced hypotension significantly decreased, as did the numerator coefficients of the AR model and transfer function gain. Conclusions: 1) Beat-to-beat HR responses to dynamic changes in ABP may be controlled by an error signal rather than directional changes in pressure, suggesting a "set point" mechanism in short-term ABP control. 2) The quantitative relationship between dynamic changes in ABP and HR can be described by a second-order AR model with a pure time delay. 3) The ability of the baroreflex to evoke a HR response to transient changes in pressure was reduced during LBNP, which was due primarily to a reduction of the static gain of the baroreflex. 相似文献
10.
Raed Salim Gali Garmi Zohar Nachum Eliezer Shalev 《Reproductive biology and endocrinology : RB&E》2010,8(1):81