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Transient receptor potential vanilloid 1 receptors (TRPV1) play a significant physiological role. The study of novel TRPV1 agonists and antagonists is essential. Here, we report on the characterization of polypeptide antagonists of TRPV1 based on in vitro and in vivo experiments. We evaluated the ability of APHC1 and APHC3 to inhibit TRPV1 using the whole-cell patch clamp approach and single cell Ca2+ imaging. In vivo tests were performed to assess the biological effects of APHC1 and APHC3 on temperature sensation, inflammation and core body temperature. In the electrophysiological study, both polypeptides partially blocked the capsaicin-induced response of TRPV1, but only APHC3 inhibited acid-induced (pH 5.5) activation of the receptor. APHC1 and APHC3 showed significant antinociceptive and analgesic activity in vivo at reasonable doses (0.01–0.1 mg/kg) and did not cause hyperthermia. Intravenous administration of these polypeptides prolonged hot-plate latency, blocked capsaicin- and formalin-induced behavior, reversed CFA-induced hyperalgesia and produced hypothermia. Notably, APHC3’s ability to inhibit the low pH-induced activation of TRPV1 resulted in a reduced behavioural response in the acetic acid-induced writhing test, whereas APHC1 was much less effective. The polypeptides APHC1 and APHC3 could be referred to as a new class of TRPV1 modulators that produce a significant analgesic effect without hyperthermia.  相似文献   
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微生境构建被广泛应用于沙化生态系统恢复的研究中,但是极少研究关注微生境构建对高寒沙化地的恢复作用,这对高寒沙漠化生态防治极为不利。为此,在川西北高寒沙地上,引种俄罗斯大果沙棘构建单株和团块微生境用于沙化生态治理研究,探究微生境构建3年对微生境中植物类型和多样性的影响,对土壤容重、含水量、pH、有机碳、全氮、全磷、微生物生物量碳、氮、磷的影响,明确微生境构建对地上和土壤生态系统的促进效应。结果表明:构建微生境增加了灌丛和草本群落盖度,团块微生境显著增加了群落物种多样性,丰富了不同生态类型的植物种类,但构建微生境并没有改变群落优势物种;构建微生境并没有显著改善土壤容重、含水量、pH;团块微生境使土壤有机碳增加至5.55 g/kg,全氮增加至0.35 g/kg,全磷增加至0.69 g/kg,并且也显著增加了土壤微生物生物量;但是高寒沙地土壤养分依然贫瘠,需要长期的恢复来改善养分条件。大果沙棘构建的团块微生境对高寒沙地的恢复效果优良,在进行高寒沙地修复过程中,建议利用灌丛构建团块微生境来进行生态恢复。  相似文献   
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Graphocephala fennahi Young, 1977 (Cicadellidae) was observed for the first time in Russia in 2018 in Moscow City on hedge bindweed, Calystegia sepium (Convolvulaceae) and Rhododendron spp. (Ericaceae). A small population of Pochazia shantungensis (Chou & Lu, 1977) (Ricaniidae) was recorded for the first time in Russia in 2022 in Sochi City, Krasnodar Territory, on the broad-leaf privet, Ligustrum lucidum (Oleaceae). It is likely that both species of insects were accidentally introduced with ornamental plants for planting. In total, alien Auchenorrhyncha species in Russia now comprise six species, two of which are of Asian origin (Orosanga japonica and P. shantungensis; both Ricaniidae) and four are of Nearctic origin (Stictocephala bisonia [Membracidae], Metcalfa pruinosa [Flatidae], Scaphoideus titanus and G. fennahi [both Cicadellidae]).  相似文献   
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-  Dedicated to Prof. Dr. Ulrich Förstner on his 65th birthdayBackground   Surface complexation models (SCM) alone have yet less successfully reproduced sorption isotherms of hydrous manganese oxides (HMO). This is in part due to the fact that the HMO structure may vary with pH, and also because microbially formed natural HMO has an oxidation number O/Mn 〈 2, i.e. is of non-stoichiometrical composition. The former effect has often led to severe artefacts, such as an under-prediction of metal sequestration at low pH, and non-comparable pK and pHZPC values in literature. The latter effect is of particular importance for environments of varying redox conditions like sediments.Objectives   We propose therefore a new sorption model comprising of amphoteric site SCM, ion exchange due to permanent charge compensation, and solid solution formation, in order to comply at least in part with the redox complexity of HMO phases of stable birnessite- and buserite-type structures. Methods   The model is run by a new Gibbs energy minimization code which is shown to be particularly suitable for such a sorption continuum approach. Results and Discussion   Initial calibration of the model was performed by experimental literature data on simple laboratory systems. Thus parameterised, we simulated on the basis of available field data the effect of redox-driven dissolution of a ferromanganese nodule on the partitioning of metals between the interacting HMO, HFO, and marine water phases. Our scenario model suggests that significant fraction of Mn and other metals, probably 50% or more, may be recycled to water column from the surface of the ferromanganese nodule upon gradual development of the bottom water stagnation, except of Zn for which a by far stronger net retention was found.Conclusion and Outlook   Our model, even if only a first approximation, clearly shows that stagnation in the marine bottom water, once occurring, can drastically change primary element proxy records in ferromanganese nodules, smoothing out any anomalous patterns in the most recent record.  相似文献   
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