Tachykinin NK-1 receptor probed with constrained analogues of substance P

The action of rotameric probes introduced either in position 7 or 8 in the sequence of substance P (SP) was investigated, i.e. -tetrahydroisoquinoleic acid (Tic), -fluorenylglycine (Flg), -diphenylalanine (Dip), the diastereoisomers of -1-indanylglycine (Ing) and -benz[ƒ]indanylglycine (Bfi), the Z- and E-isomers of dehydrophenylalanine and dehydronaphthylalanine (Δ^ZPhe, Δ^EPhe, Δ^ZNal, Δ^ENal) and (Dmp). The aim of this study was the topographical characterization of the binding subsites of human NK-1 receptor expressed in CHO cells, especially the S₇ and S₈ subsites, corresponding to residues Phe⁷ and Phe⁸ of substance P. According to the binding potencies of these substituted-SP analogues, the S₇ binding subsite is smaller than the S₈ subsite: the S₇ subsite accepts only one aromatic nucleus, while the S₈ can accommodate three coplanar nuclei altogether. These findings are compatible with the idea that the S₈ binding subsite may reside in the extracellular loops of the hNK-1 receptor. NK-1 agonists bind to human NK-1 receptor and activate the production of both inositol phosphates and cyclic AMP. As already quoted for septide, [pGlu⁶, Pro⁹]SP(6–11), discrepancies are observed between affinity (K_i) and activity (EC₅₀) values for IPs production. While a weak correlation between K_i and EC₅₀ values for IPs production could be found (r = 0.70), an excellent correlation could be demonstrated between their affinities (K_i) and their potencies (EC₅₀) for cAMP production (r = 0.97). The high potency (EC₅₀) observed for ‘septide-like’ molecules on PI hydrolysis, compared to their affinity is not an artefact related to the high level of NK-1 receptors expressed on CHO cells since a good correlation was found between EC₅₀ values obtained for PI hydrolysis and those measured for spasmogenic activity in guinea pig ileum bioassay (r = 0.94).

According to the binding potencies of constrained analogues of phenylalanine, the S₇ binding subsite of human NK-1 receptor is small, whereas the S₈, which can accommodate three coplanar nuclei, might probably reside in the extracellular loop. The discrepancies observed between affinity (K_i) and activity (EC₅₀) values for IPs production are not an artefact of CHO cells since a good correlation was found between EC₅₀ for PI hydrolysis and those measured in guinea pig ileum bioassay.     

陕西省第一批国家稀有濒危植物的地理分布、区系特征及保护

分析了陕西省稀有濒危植物４６个种（包括种下等级）的地理分布和４２个属的分布区类型及其区系特征,提出了稀有濒危植物种质资源的保护对策。     

庐山野生观赏植物资源多样性及持续利用对策

庐山是我国著名的风景旅游和避暑胜地,也是我国中亚热带北缘植物多样性的宝库．本文在广泛调查、收集、整理的基础上,研究了庐山野生观赏植物资源多样性特征、分布、类型及其配置．本区分布有野生观赏植物５２８种,隶属于１１５科２９０属,其中乔木类１３８种,灌木类１４０种,藤木类５２种,草本类１９８种．并根据开发与保护现状对庐山野生观赏植物资源多样性的持续利用提出了切实可行的对策．     

苯甲醛对果蝇视觉联想记忆的阻断

采用飞行模拟系统,以视觉模式为线索、热惩罚为负强化因子,对于在不同发育时期经受苯甲醛处理过的果蝇的视觉飞行定向条件化进行了检验。苯甲醛气味分别作用于果蝇幼虫和成虫阶段,将阻断果蝇成虫建立视觉联想记忆的能力;雌性果蝇在处女期对苯甲醛气味的接触,会阻断其子代建立视觉联想记忆,这种视觉联想记忆的能力可以通过对其子代连续３代的正常饲养而逐渐得到恢复。     

癫痫对大鼠学习记忆的影响及与生长抑素的相关性研究

对听源性癫痫大鼠进行迷宫训练,观察癫痫发作对大鼠光分辨学习作业的成绩以及用放射免疫分析法测定的大鼠部分脑区中生长抑素含量的影响。结果表明：（１）癫痫发作对大鼠记忆阶段有明显的抑制作用（Ｐ＜０．０１）;（２）癫痫发作后,在大鼠信息提取明显障碍的同时,其颞叶皮层、下丘脑、垂体及海马中生长抑素的含量明显增加（Ｐ＜０．０５－０．０１）。结果提示：癫痫发作影响大鼠学习记忆过程,在该过程中生长抑素含量发生改变。     

盐或低温胁迫对花生幼苗下胚轴ATP酶和质膜中PIP2含量的影响

经６％－１２％Ｄｅｘｔｒａｎ Ｔ７０密度梯度离心,获得了纯度较高的７ｄ龄花生幼苗下胚轴质膜和液泡膜制剂。１５０ｍｍｏｌ／Ｌ ＮａＣｌ或１０℃低温处理花生幼苗２４ｈ,其下胚轴质膜上的Ｍｇ＾２＋激活的ＡＴＰａｓｅ活性分别提高了３７．６％和１７．２％;Ｃａ＾２＋－ＡＴＰａｓｅ活性分别提高４５．８％和３３．６％。上述盐或低温处理也提高了液泡膜上Ｍｇ＾２＋激活的ＡＴＰａｓｅ活性,分别为对照的１４１．２％和１     

真菌诱导子对悬浮培养西洋参细胞的生理效应

报道了不同真菌诱导子对悬浮培养的西洋参（Ｐａｎａｘｑｕｉｎｑｕｅｆｏｌｉｕｍ）细胞生长、皂甙和多糖合成,以及细胞内和培养液中过氧化物酶活性的生理效应。悬浮培养的西洋参细胞经刺盘孢菌（Ｃｏｌｌｅｔｏｔｒｉｃｈｕｍｎｉｃｏｌｔｉａｎａｅ）丝体诱导子处理后,总皂甙产率可由对照的２９６ｍｇ／Ｌ增加到６７９ｍｇ／Ｌ（约占细胞干重的（１６．３％）,比对照提高约１．３倍,而且总皂甙的８５％排放在培养液中;经黑曲霉（Ａｓｐｅｒｇｉｌｌｕｓｎｉｇｒａｎ）诱导子处理后,细胞多糖含量可达到１１．７９％（细胞干重）,比对照增加１倍多。初步纯化的刺盘孢菌丝体诱导子和尖孢镰刀菌（Ｆｕｓｕｒｉｕｍｏｘｙｓｐｏｒｕｍ）滤液诱导子在诱导处理前期能明显促进西洋参细胞生长,同时细胞内及培养液中过氧化物酶活性显著增加;随时间延长,细胞生长和酶活性逐步受到抑制。     

一类竞争扩散方程组在Neumann边条件下解的渐近行为

本文主要采用比较方法讨论了一类竞争扩散方程组在Neumann边条件下解的渐近行为,得到了解的稳定性区域．     

多组多滞后区间系数定常非线性关联控制大系统的结构与关联鲁棒镇定(I)

建立了多组多滞后区间系数定常非线性控制系统的结构概念,采用鲁棒镇定的等价法,给出了具有扰动结构参数的多组多滞后区问系数定常非线性关联控制大系统的结构与关联鲁棒镇定,同时给出了扰动参数与滞后非线性项界线的估价公式。     

豆田刺吸类害虫、天敌自然种群消长规律及其群落结构的研究

在豆田群落中,常见的天敌昆虫及有益生物为12科13种,它们对寄主均有很强的选择性．小花蝽是大豆蚜的主要天敌,系优势种,其次是龟纹瓢虫．大青叶蝉的主要天敌是蜘蛛类,三突花蛛和草间小黑蛛为优势种．在长期不施用农药的环境下,天敌自然种群对控制害虫发生危害的作用明显．经数学分析,建立了12个数学模型,进一步揭示了两种刺吸类害虫与其天敌之间的关系;天敌种群消长、害虫种群消长与时间变动的关系．尤其通过对豆田群落生物的多样性、稳定性动态分析,表明豆田群落在8月9日至8月29日多样性指数和稳定性指数最大;同时亦表明豆田群落的多样性指数愈高,群落的稳定性愈强．