共查询到20条相似文献，搜索用时 15 毫秒
1.
Interaction of convulsive ligands with benzodiazepine receptors 总被引：40，自引：0，他引：40
C Braestrup R Schmiechen G Neef M Nielsen E N Petersen 《Science (New York, N.Y.)》1982,216(4551):1241-1243
The gamma-aminobutyric acid (GABA)-benzodiazepine receptor complex, which is composed of distinct proteins embedded in the neuronal plasma membrane, is important for several effects of benzodiazepines, including protection afforded against convulsions. During structural modification of ethyl beta-carboline-3-carboxylate an agent was discovered which has high affinity for brain benzodiazepine receptors but which is a potent convulsant. Also in contrast to benzodiazepines, this type of benzodiazepine receptor ligand favors benzodiazepine receptors in the non-GABA-stimulated conformation, which may explain the convulsive properties. 相似文献
2.
超声波辐射合成香豆素-3-甲酸乙酯 总被引：1，自引：0，他引：1
[目的]利用超声波辐射技术合成香豆素-3-甲酸乙酯,并优化其反应条件。[方法]采用超声波辐射技术,经Knoevenagel缩合反应合成了香豆素-3-甲酸乙酯,产物经IR1、HNMR表征。通过单因素优选法研究了不同水杨醛和丙二酸二乙酯投料比例、反应温度、辐射时间、无水乙醇用量、六氢吡啶用量对反应产率的影响。[结果]超声波辐射法制备香豆素-3-甲酸乙酯的最佳合成条件：水杨醛与丙二酸二乙酯物质的量之比为1.001∶.30,无水乙醇25 ml,六氢吡啶0.5 ml,在65℃下,超声波辐射作用80 min,产率达97.46%。[结论]与传统法相比,该合成方法缩短了反应时间,较常规方法产率提高了近20个百分点。 相似文献
3.
GABAA (gamma-aminobutyric acid A)-benzodiazepine receptors expressed in mammalian cells and assembled from one of three different alpha subunit variants (alpha 1, alpha 2, or alpha 3) in combination with a beta 1 and a gamma 2 subunit display the pharmacological properties of either type I or type II receptor subtypes. These receptors contain high-affinity binding sites for benzodiazepines. However, CL 218 872, 2-oxoquazepam, and methyl beta-carboline-3-carboxylate (beta-CCM) show a temperature-modulated selectivity for alpha 1 subunit-containing receptors. There were no significant differences in the binding of clonazepam, diazepam, Ro 15-1788, or dimethoxy-4-ethyl-beta-carboline-3-carboxylate (DMCM) to all three recombinant receptors. Receptors containing the alpha 3 subunit show greater GABA potentiation of benzodiazepine binding than receptors containing the alpha 1 or alpha 2 subunit, indicating that there are subtypes within the type II class. Thus, diversity in benzodiazepine pharmacology is generated by heterogeneity of the alpha subunit of the GABAA receptor. 相似文献
4.
5.
8-甲氧基-香豆素-3-甲酸香叶酯的合成及在卷烟中的应用 总被引：1，自引：1，他引：1
采用酰氯酯化法,以8-甲氧基-香豆素-3-甲酸与香叶醇为原料合成了8-甲氧基-香豆素-3-甲酸香叶酯,经IR,HRMS,~1H NMR,~(13)C NMR等鉴定,证实了其结构.采用热解-GC/MS对热解产物进行了分离鉴定,并对8-甲氧基-香豆素-3-甲酸香叶酯进行了卷烟加香试验.结果表明,600℃时,8-甲氧基-香豆素-3-甲酸香叶酯的热解产物中共鉴定出27种成分,主要为烯类、烷类、酸类、醇类、酚类;鉴定出香叶醇,且相对峰面积3.6,说明8-甲氧基-香豆素-3-甲酸香叶酯能在卷烟燃吸温度下释放出一定量的香叶醇;8-甲氧基-香豆素-3-甲酸香叶酯具有改善和修饰卷烟香气,增加甜韵和豆香香韵,减轻刺激性的作用. 相似文献
6.
Receptors for the age of anxiety: pharmacology of the benzodiazepines 总被引：40，自引：0，他引：40
Investigation of the actions of the benzodiazepines has provided insights into the neurochemical mechanisms underlying anxiety, seizures, muscle relaxation, and sedation. Behavioral, electrophysical, pharmacological, and biochemical evidence indicates that the benzodiazepines exert their therapeutic effects by interacting with a high-affinity binding site (receptor) in the brain. The benzodiazepine receptor interacts with a receptor for gamma-aminobutyric acid, a major inhibitory neurotransmitter, and enhances its inhibitory effects. The benzodiazepine receptor may also interact with endogenous substances and several naturally occurring compounds, including the purines and nicotinamide, are candidates for this role. Both the purines and nicotinamide possess some benzodiazepine-like properties in vivo, although further work will be required to confirm their possible roles as endogenous benzodiazepines. 相似文献
7.
以薄荷醇和8-甲氧基香豆素-3-甲酸为原料,合成了一种新型、释放型清凉剂8-甲氧基香豆素-3-甲酸薄荷酯,产物的结构经IR、1H NMR、13C NMR和HRMS确证.采用在线裂解气相色谱-质谱联用技术,对8-甲氧基香豆素-3-甲酸薄荷酯在600℃下的裂解行为进行了研究,并对8-甲氧基香豆素-3-甲酸薄荷酯进行了卷烟加香试验.结果表明:(1)600℃时,香豆素-3-甲酸薄荷酯的热解产物中共鉴定出25种成分,其中多种为重要的烟草香味成分;(2)8-甲氧基香豆素-3-甲酸薄荷酯具有改善和修饰卷烟烟气,增加豆香与清凉香气,减轻刺激性的作用. 相似文献
8.
[目的]分析橘小实蝇引诱蛋白——啤酒废酵母酶解液的挥发性成分。[方法]采用固相微萃取法(SPME)收集新鲜啤酒废酵母水解蛋白中的挥发性成分,并气质联用仪(GC-MS)对其进行了分析。[结果]鉴定出乙醇、丙酮3、-甲基-1-丁醇、甲氧基-苯基-肟、苯甲醛、己酸、苯乙醇、苯乙腈、辛酸、辛酸乙酯、乙酸辛酯、甲酸苯乙酯、壬酸乙酯9、-烯癸酸乙酯、癸酸乙酯和十二烷酸乙酯共16种物质,其中乙醇、丙酮3、-甲基-1-丁醇、苯甲醛、苯乙醇、己酸、辛酸和辛酸乙酯曾被不同学者在实蝇其他食物诱剂中发现,且乙醇和辛酸乙酯已被证实对一些实蝇种类具有引诱活性,未见其他8种物质在实蝇食物诱剂中的检出报道。[结论]为该实蝇蛋白诱剂的进一步改良提供了理论依据。 相似文献
9.
Analysis of Volatile Components in Strawberry Cultivars Xingdu 1 and Xingdu 2 and Their Parents 总被引：1，自引：0，他引：1
ZHANG Yun-tao WANG Gui-xia DONG Jing ZHONG Chuan-fei KONG Jin LI Tian-zhong HAN Zhen-hai 《中国农业科学(英文版)》2009,8(4):441-446
To study differences and genetic trends of volatiles in Xingdu 1 and Xingdu 2, the strawberry cultivars, with their parents, the volatile components were analyzed by head space-solid phase microextraction and gas chromatography-mass spectrometry. The results indicated that a total of 50 compounds were identified in Xingdu 1 cultivar, including hexanoic acid methyl ester and hexanoic acid ethyl ester, butanoic acid methyl ester, and butanoic acid ethyl ester, octanoic acid methyl ester and octanoic acid ethyl ester, isomyl hexanoate. And there were 71 compounds in Xingdu 2, which were similar to that of Xingdu 1. About 55 volatiles were identified in Allstar （female parent）, including acetone, acetic acid 1- methylethyl ester, 1-octanol, hexanoic acid ethyl ester and butanoic acid methyl ester. And 43 volatiles were identified in Toyonoka （male parent）, including hexanoic acid ethyl ester, nerolidol, 1-octanol, hexanoic acid methyl ester, acetic acid octyl ester, isomyl hexanoate and octanoic acid methyl ester. Consequently, hexanoic acid methyl ester and hexanoic acid ethyl ester, butanoic acid methyl ester, and butanoic acid ethyl ester and isomyl hexanoate in twins might be affected both sides of their parents. In the family, male parent （Toyonoka） had the highest concentrations of fragrance alcohols, such as nerolidol, linalool and 1-octanol, but which couldn＇t be transmitted to the descendants. Acetone, acetic acid 1- methylethyl ester of the twins originally came from matrilinear inheritance, as the contents of the two compounds were very high in Allstar but little in Toyonoka. Genetic trends of butanoic acid methyl ester, butanoic acid ethyl ester, hexanoic acid ethyl ester, hexanoic acid methyl ester and isomyl hexanoate were affected by both sides of parents. 相似文献
10.
P D Suzdak J R Glowa J N Crawley R D Schwartz P Skolnick S M Paul 《Science (New York, N.Y.)》1986,234(4781):1243-1247
Ethanol, at pharmacologically relevant concentrations of 20 to 100 mM, stimulates gamma-aminobutyric (GABA) receptor-mediated uptake of 36Cl-labeled chlorine into isolated brain vesicles. One drug that acts at GABA-benzodiazepine receptors, the imidazobenzodiazepine Ro15-4513, has been found to be a potent antagonist of ethanol-stimulated 36Cl- uptake into brain vesicles, but it fails to antagonize either pentobarbital- or muscimol-stimulated 36Cl- uptake. Pretreatment of rats with Ro15-4513 blocks the anticonflict activity of low doses of ethanol (but not pentobarbital) as well as the behavioral intoxication observed with higher doses of ethanol. The effects of Ro15-4513 in antagonizing ethanol-stimulated 36Cl- uptake and behavior are completely blocked by benzodiazepine receptor antagonists. However, other benzodiazepine receptor inverse agonists fail to antagonize the actions of ethanol in vitro or in vivo, suggesting a novel interaction of Ro15-4513 with the GABA receptor-coupled chloride ion channel complex. The identification of a selective benzodiazepine antagonist of ethanol-stimulated 36Cl- uptake in vitro that blocks the anxiolytic and intoxicating actions of ethanol suggests that many of the neuropharmacologic actions of ethanol may be mediated via central GABA receptors. 相似文献
11.
通过GC-MS分析,从华莱士瓜果实中检出45种不同成分的芳香物质。主要的物质为软脂酸、亚麻酸、亚油酸、油酸、顺-十六碳烯酸、二十八烷、二十三烷、乙酸-3-甲基丁酯、乙酸苯甲酯、3-羟基-2-丁酮、二十七烷、硬脂酸、乙酸乙酯、乙酸丙酯、乙酸-2-甲基丙酯、丁酸乙酯、乙酸丁酯、乙酸-2-甲基丁酯、2,2'-甲二氧基丙烷、2-甲基丙基肼、苯甲醇21种物质,占芳香物质总含量的71%。 相似文献
12.
The binding of [3H]diazepam to benzodiazepine receptors was studied in extensively washed membranes of rat cerebral cortex in the presence of the depressant barbiturate, pentobarbital. Pentobarbital, like the endogenous neurotransmitter gamma-aminobutyric acid (GABA), increased the basal binding and also potentiated the GABA-enhanced binding of [3H]diazepam to benzodiazepine receptors by increasing the apparent affinity of [3H]diazepam for the benzodiazepine receptor. The concentrations of pentobarbital necessary to elicit these effects in vitro are the same as those observed after treatment with pharmacologically relevant doses, suggesting that a common neurochemical association may exist between these types of compounds. 相似文献
13.
A peptide having enzyme-like catalytic activity has been designed and synthesized. Computer modeling was used to design a bundle of four short parallel amphipathic helical peptides bearing the serine protease catalytic site residues serine, histidine, and aspartic acid at the amino end of the bundle in the same spatial arrangement as in chymotrypsin (ChTr). The necessary "oxyanion hole" and substrate binding pocket for acetyltyrosine ethyl ester, a classical ChTr substrate, were included in the design. The four chains were linked covalently at their carboxyl ends. The peptide has affinity for ChTr ester substrates similar to that of ChTr and hydrolyzes them at rates approximately 0.01 that of ChTr; total turnovers greater than 100 have been observed. The peptide is inhibited by ChTr specific inhibitors and is inactive toward benzoyl arginine ethyl ester, a trypsin substrate. The peptide is inactivated by heating above 60 degrees C, but recovers full catalytic activity upon cooling and lyophilization from acetic acid. 相似文献
14.
套袋对两个苹果品种果实香气成分的影响 总被引：1，自引：0，他引：1
为了解套袋对苹果品种新富1号(Malus domestica Borkh.cv.Xinfu No.1)、长富2号(M.domestica cv.Fuji Nagafu No.2)果实香气成分的影响。利用顶空固相微萃取和气相色谱-质谱联用技术,分别测定了套袋后2个苹果品种的香气成分。结果表明,2个富士苹果品种果实香气成分均以酯类和醇类化合物为主。在酯类化合物相对含量上,未套袋果实套袋果实;在醇类化合物相对含量上,套袋果实未套袋果实。新富1号果实香气成分以乙酸乙酯、乙酸丁酯、2-甲基乙酸丁酯、丁酸乙酯、乙酸己酯为主,长富2号果实香气成分以2-甲基乙酸丁酯、乙酸己酯、正戊酸己酯、2-甲基-1-丁醇、丁酸乙酯、丁酸丙酯、乙酸丁酯、2-甲基丁酸乙酯、丙酸乙酯为主,2个苹果品种的果实主要香气成分基本一致。不过套袋果实乙酸酯型香气成分相对含量均低于未套袋果实。 相似文献
15.
套袋对鸭梨果实香气及糖酸组分的影响 总被引：1，自引：0，他引：1
采用静态顶空和气相色谱-质谱联用技术、高效液相色谱技术,研究了生长期套袋对鸭梨果实挥发性成分、糖酸组分等风味物质的组成和含量的影响。结果表明:套袋导致鸭梨香气物质种类减少和相对百分含量降低。套袋鸭梨采收时测定的香气成分有3类18种,其中酯类15种、烯类2种、醇类1种;不套袋鸭梨采收时测定的香气成分有3类26种,其中酯类23种、烯类2种、醇类1种。鸭梨的主要香气成分是乙酸己酯、己酸乙酯、丁酸乙酯。套袋和不套袋鸭梨均检测到3种糖、4种有机酸组分,其中糖组分主要为果糖,其次为蔗糖、葡萄糖,有机酸组分主要为苹果酸,其次为乙酸、柠檬酸、草酸,但不同处理间含量存在差异。 相似文献
16.
A benzodiazepine receptor antagonist decreases sleep and reverses the hypnotic actions of flurazepam 总被引：2，自引：0，他引：2
The benzodiazepine receptor antagonist 3-hydroxymethyl-beta-carboline, which blocks several of the pharmacological actions of benzodiazepines, induces a dose-dependent increase in sleep latency in the rat. Furthermore, at a low dose that by itself does not affect sleep, 3-hydroxymethyl-beta-carboline blocks sleep induction by a large dose of flurazepam. The benzodiazepine receptor may play a role in both the physiological regulation and pharmacological induction of sleep. 相似文献
17.
吉林地区山葡萄果实香气成分的GC/MS分析 总被引：1，自引：0，他引：1
利用固相微萃取和气质质谱联用技术,对吉林地区山葡萄代表品种双优、双红、左优红果实的香气成分进行了GC/MS检测分析,并结合计算机检索技术对分离化合物进行了鉴定,应用TIC峰面积归一法测定了各成分的相对含量。结果发现,双优、双红、左优红果实中分别含有45,47和48种香气物质,分别占各自所有组分总峰面积的87.93%,74.76%和95.74%;3种山葡萄主要果香成分有乙酸乙酯、己酸乙酯、橙花醇乙酸酯、乙酸苯乙酯、异丁醇、3-甲基丁醇、正己醇、2-辛醇、苯乙醇、香茅醇、里哪醇、2-辛酮和苯醛等。 相似文献
18.
氮素处理对成熟草莓果实芳香成分的影响 总被引：6，自引：0，他引：6
采用溶剂萃取法提取经不同氮素水平处理后的成熟草莓果实芳香成分，进行气相色谱-质谱联用仪(GC／MS)分析。结果表明：高量氮肥、中量氮肥、低量氮肥、不施氮肥四个处理分别检测出27种、29种、28种、26种芳香成分，各占总峰面积的94．01％，91．45％，94．79％，94．53％。各处理成熟草莓果实中特征芳香成分丁酸甲酯、丁酸乙酯、己酸甲酯、2，5-二甲基-4-羟基-3(2H)-呋喃酮、2，5-二甲基-4-甲氧基-3(2H)-呋喃酮等的相对含量存在差异；中量氮肥处理时特征香气成分总含量最高，不施氮肥时总含量最低。 相似文献
19.
Presence of nonoxidative ethanol metabolism in human organs commonly damaged by ethanol abuse 总被引：18，自引：0，他引：18
Acetaldehyde, the end product of oxidative ethanol metabolism, contributes to alcohol-induced disease in the liver, but cannot account for damage in organs such as the pancreas, heart, or brain, where oxidative metabolism is minimal or absent; nor can it account for the varied patterns of organ damage found in chronic alcoholics. Thus other biochemical mediators may be important in the pathogenesis of alcohol-induced organ damage. Many human organs were found to metabolize ethanol through a recently described nonoxidative pathway to form fatty acid ethyl esters. Organs lacking oxidative alcohol metabolism yet frequently damaged by ethanol abuse have high fatty acid ethyl ester synthetic activities and show substantial transient accumulations of fatty acid ethyl esters. Thus nonoxidative ethanol metabolism in addition to the oxidative pathway may be important in the pathophysiology of ethanol-induced disease in humans. 相似文献
20.
固相微萃取分析发酵肉制品中的挥发性风味组分 总被引：7，自引：0，他引：7
为开发新型肉制品,运用SPME-GC-MS对传统侗族发酵肉制品中的挥发性风味组分进行了分析.结果表明,在鉴定出的48种风味物质中,酯、醛、醇、烷烃分别为13,11,6,5种,其他杂环化合物13种.主体风味成分是己酸乙酯、苯乙醇、辛酸和辛酸乙酯. 相似文献