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Novel alternative splicing of GABA receptor RDL exon 9 from Laodelphax striatellus modulates agonist potency
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作者 Jie Jiang Li-Xin Huang +4 位作者 Feng Chen Cheng-Wang Sheng Qiu-Tang Huang Zhao-Jun Han Chun-Qing Zhao 《Insect Science》 SCIE CAS CSCD 2021年第3期757-768,共12页
The resistance to dieldrin gene(RDL)encodes the primary subunit of the insect ionotropic y-aminobutyric acid(GABA)receptor(GABAR),which is the target of phenylpyrazole and isoxazoline insecticides.The splice variants ... The resistance to dieldrin gene(RDL)encodes the primary subunit of the insect ionotropic y-aminobutyric acid(GABA)receptor(GABAR),which is the target of phenylpyrazole and isoxazoline insecticides.The splice variants in exons 3 and 6 of RDL,which have been widely explored in many insects,modulate the agonist potency of the homomeric RDL GABAR and potentially play an important role in the development of insects.In the present study,four splice variants of exon 9 were identified in RDL of the small brown planthopper,Laodelphax striatellus(LsRDL),resulting in LsRDL-9sl,LsRDL-92l\LsRDL-9b,and LsRDL-9c.LsRDL-9a has one more amino acid(E,glutamic acid)compared with LsRDL-9a\and LsRDL-9b lacked two amino acids and had seven different amino acids compared with LsRDL-9c.Two-electrode voltage-clamp recording on LsRDLs expressed in Xenopus oocytes showed that alternative splicing of exon 9 has significant impact on LsRDL sensitivity to the agonists GABA and 0-alanine,whereas no significant difference was observed in the potencies of the non-competitive antagonists(NCAs)ethiprole and fluralaner on the splice variants.Our results suggest that alternative splicing of RDL exon 9 broadens functional capabilities of the GABAR in L.striatellus by influencing the action of GABA. 展开更多
关键词 alternative splicing exon 9 gaba receptor Laodelphax striatellus^RDL
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GetArtemisininsByAnymeans (GABA): artemisinins path to conquer diabetes go through GABA receptors
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作者 Xiaojie Bai Suneng Fu 《Science Bulletin》 SCIE EI CAS CSCD 2017年第6期383-385,共3页
Diabetes is a chronic disease of elevated blood glucose levels that affects more than 400 million people worldwide.Complications of diabetes affect the neuronal and the vascular systems and causes diabetic kidney dise... Diabetes is a chronic disease of elevated blood glucose levels that affects more than 400 million people worldwide.Complications of diabetes affect the neuronal and the vascular systems and causes diabetic kidney disease,cardiovascular disease,hypertension,retinopathy,peripheral neuropathy,and diabetic food diseases.Diabetes is caused by either the body’s inability to 展开更多
关键词 gaba cell artemisinins path to conquer diabetes go through gaba receptors Get Artemisinins By Anymeans
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Ultrasound combined blood-brain barrier targeting brain delivery of four-in-one molecular aggregates for the enhancement of anesthetic efficacy and toxicity reduction via propofol-etomidate synergistically inhibition GABA receptor
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作者 Shuo Zhang Yishu Wang +11 位作者 Mingting Zhu Bingyang Liu Wenpu Zhao Shuai Zhang Ji Xia Lei Shi Peng Tang Feiqian Wang Siyuan Zhang Mingxi Wan Daocheng Wu Wei Gao 《Aggregate》 EI CAS 2024年第5期245-264,共20页
To enhance the anesthetic efficacy and reduce toxic side effects,a strategy is proposed involving the utilization of general anesthetics of Propofol(Pro)and Eto-midate(Eto)to synergistic inhibition GABA receptors simul... To enhance the anesthetic efficacy and reduce toxic side effects,a strategy is proposed involving the utilization of general anesthetics of Propofol(Pro)and Eto-midate(Eto)to synergistic inhibition GABA receptors simultaneously.Four-in-one molecular aggregates were prepared to implement this strategy,which comprised of Pro and Eto with the bridging molecule monoglyceride monooleate(GMO)and sur-factant F127 through intermolecular forces.The blood-brain barrier(BBB)targeted lactoferrin(LF)is affixed to their surface,obtaining thefinal molecular aggregates.By employing lactoferrin enrich aggregates to the BBB,followed by ultrasound combine microbubbles to open the BBB,a remarkable 4.5-fold enhancement in brain drug delivery was achieved.The molecular aggregates group maintained sta-ble parameters of heart rate,diastolic blood pressure,and systolic blood pressure.A notable increase of more than twice therapeutic index(TI)value was observed,implying their higher anesthesia efficiency and reduced toxicity.Electroencephalo-gram(EEG)experiments demonstrate a significant elevation in the proportion of θ waves from 28%to 80%for aggregates,accompanied by a nearlyfivefold reduc-tion in the proportion ofθwaves,meaning a significant improvement in synergistic anesthesia effectiveness(interaction index 0.289)with lower drug dosage.Further-more,mouse immunofluorescence brain slice experiments suggest Pro and Eto enter the GABA receptor simultaneously,resulting in synergistic inhibition of GABA receptors. 展开更多
关键词 blood-brain barrier brain delivery gaba receptor molecular aggregates synergistic anesthetic efficacy
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Preliminary Study on γ-Aminobutyric Acid (GABA_A) Like Receptor in Rat Testis
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作者 杨绍华 严缘昌 +2 位作者 武玮磷 胡菁华 陈小章 《Journal of Reproduction and Contraception》 CAS 1998年第1期27-33,共7页
For making it clear whether GABAA-like receptor is in cells or rat testis and how itsgene expresses in tissue cells, the mRNA of rat testis was microinjected into Xenopusoocyte. The membrane electrobiological results ... For making it clear whether GABAA-like receptor is in cells or rat testis and how itsgene expresses in tissue cells, the mRNA of rat testis was microinjected into Xenopusoocyte. The membrane electrobiological results showed that an inward 30 nA micro-currentwas elicited, under two-electrode voltageclamped configuration, by extracellular GABA(500 μmol/L), and both Bicuculline and Picrotoxin could inhibit this effect. It is an indication that the mRNA of rat testis can express GABA receptor in the membrane of Xenonpus oocyte. Using Muscimol as a excitant of GABA receptor type A, the micro--currentwas also elicited to generate; however, using Baclofen as a excitant of GABA receptortype B, the micro-current could not be induced. These results indicate that GABA receptorexpressed in Xenopus oocyte membrane is not type B but for type A. On the basis of the research result above, 24-mer oligonucleotides to be complementary to the high conservativeregion of the cDNAs of neur-GABA receptors were synthesized as probes to hybridize respectively with the RNAs Of brain and testis of adult rat, and of rat testes of the variousages. The dot hybridizations showed that the hybrid signal of rat testis was stronger thanthat of rat brain, meaning that, compared with rat brain, the RNA of rat testis has morehomologous regions with probes, and also implying that the GABA receptor from theRNA Of rat testis may be similar to neural-GABA receptor. This receptor therefore iscalled as GABA_A-like receptor. The dot blot analysis above also showed the testis GABA_Alike receptor. The dot blot analysis above also showed testis GABA_A like receptor mRNAcontent changed with the develOPmental age of rats. There is a very low level of gene expression in the rat testis on day 5 postnatal; there is the highest expression of GABA_A-likereceptor gene in rat testes on day 30to 100 after birth; the expression begins to drop on day200 after birth. 展开更多
关键词 gaba receptor Rat testis mRNA Xenopus oocyte Dot hybridization Voltage-clamped configuration
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Modulation of firing activity by endogenous GABA_A receptors in the globus pallidus of MPTP-treated parkinsonian mice 被引量:1
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作者 Xin-Yi Chen Yan Xue +3 位作者 Hua Wang Su-Hong Zhu Xiao-Meng Hao Lei Chen 《Neuroscience Bulletin》 SCIE CAS CSCD 2013年第6期701-707,共7页
The globus pallidus in rodents,equivalent to the external segment of the globus pallidus in primates,plays an important role in movement regulation.Previous studies have shown abundant γ-aminobutyric acid(GABA)ergi... The globus pallidus in rodents,equivalent to the external segment of the globus pallidus in primates,plays an important role in movement regulation.Previous studies have shown abundant γ-aminobutyric acid(GABA)ergic innervation and GABAA receptors in the globus pallidus.In this study,we investigated the effects of endogenous GABAA receptors on the spontaneous firing activity of pallidal neurons in both normal and MPTP-treated mice using multi-barrel electrodes extracellular recordings in vivo.We found that in normal mice,pressure ejection of 0.1 mmol/L gabazine,a specific GABA A receptor antagonist,increased the spontaneous firing rate of globus pallidus neurons by 27.6 ± 5.6%.Furthermore,in MPTP mice(14 days after MPTP treatment),0.1 mmol/L gabazine increased the firing rates by 51.0 ± 7.9%,significantly greater than in normal mice.These results suggest that endogenous GABAA receptors modulate the activity of globus pallidus neurons.The present findings may provide a rationale for investigations into the potential role of GABAA receptors in Parkinson’s disease. 展开更多
关键词 globus pallidus gaba A receptor Parkinson’s disease single unit recording
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Electroacupuncture (EA) Speeds Up the Regulation of Hypothalamic Pituitary Adrenal Axis Dysfunction in Acute Surgical Trauma Rats: Mediated by Hypothalamic Gamma-Aminobutyric Acid (GABA)<sub>A</sub>Receptors 被引量:1
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作者 Liting Zhu Jing Zhu +5 位作者 Zhejun Chen Zehui Meng Mingda Ju Mizhen Zhang Gencheng Wu Zhanzhuang Tian 《Journal of Behavioral and Brain Science》 2018年第12期697-710,共14页
Hypothalamic Corticotropin-releasing factor (CRF) directly activates the hypothalamic pituitary adrenal axis (HPA axis) during the surgical trauma induced stress response. Electroacupuncture (EA) has been demonstrated... Hypothalamic Corticotropin-releasing factor (CRF) directly activates the hypothalamic pituitary adrenal axis (HPA axis) during the surgical trauma induced stress response. Electroacupuncture (EA) has been demonstrated to have stress relieving effects in breast surgery, colorectal surgery, prostatectomy and craniotomy. This study was aimed to investigate the hypothesis that EA could regulate hypothalamic CRF in surgical trauma rats. In experiment one, Sprague-Dawley (SD) male rats were divided into intact, model (10% partial hepatectomy), sham EA and EA group. Rats from the Sham EA and EA group were stimulated at ST36-Zusanli and SP6-Sanyiniiao acupoints twice, 24 hours before the surgery and immediately after the surgery. Expressions of hypothalamic CRF and CRFR, GABA receptors, glutamate decarboxylase (GAD), serum adrenocorticotropic hormone (ACTH) and Corticosterone (CORT) were observed at 2, 4, 8 and 24 h after the surgery by radioimmunoassay (RIA), western blot, real-time PCR and immunohistochemistry. In the experiment two, SD male rats were divided into the intact, model, model + vehicle, model + L-838,417 EA and EA + L838,417 group. It was found that hypothalamus CRF, serum ACTH and CORT levels were increased in model group compared with the intact group, and those in the EA group decreased in comparison with the model group. Compared with the model group, hypothalamus-aminobutyric acid (GABA) receptor Aα3 mRNA and protein expressions of the EA group raised strikingly. In conclusion, EA alleviated surgical stress response by improving the GABA synthesis in hypothalamus, thus enhancing GABA receptors’ inhibitory regulation of the HPA axis dysfunction in rats with acute surgical trauma. 展开更多
关键词 ELECTROACUPUNCTURE HYPOTHALAMIC Pituitary Adrenal Axis γ-Aminobutyric Acid (gaba) receptor CORTICOTROPIN Releasing Factor Surgery
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Diazepam reduces synaptic GABA type areceptor availability via multiple trafficking mechanisms
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作者 Joshua M LORENZ-GUERTIN Sabyasachi DAS Tija C JACOB 《中国药理学与毒理学杂志》 CAS CSCD 北大核心 2017年第10期952-952,共1页
OBJECTIVE Investigate the effects of diazepam(DZP) on γ2 subunit containing GABA type A receptor(GABA A R) trafficking.METHODS Immunofluorescence microscopy measured surface GABA A Rs and gephyrin in rat cortical neu... OBJECTIVE Investigate the effects of diazepam(DZP) on γ2 subunit containing GABA type A receptor(GABA A R) trafficking.METHODS Immunofluorescence microscopy measured surface GABA A Rs and gephyrin in rat cortical neurons after 24 h exposure of 1.0 μmol·L^(-1) DZP.Biochemical studies of mice injected with 10 mg·kg^(-1) DZP vs vehicle were assessed for γ2 subunit and total gephyrin cortical levels 12 h post-injection.Ubiquitination of the γ2 subunit was studied by immunoprecipitation after 12 h of 1.0 μmol·L^(-1) DZP exposure.A γ2 subunit encoding an N terminal fluorogen-activating peptide and pH-sensitive green fluorescent protein(γ2 pH FAP) measured lysosomal targeting of γ2 containing GABA A Rs.RFP-gephyrin and γ2 pH FAP synaptic diffusion rates were examined using fluorescence recovery after photobleaching(FRAP).RESULTS Extrasynaptic levels of γ2 GABA A Rs decreased by 12.2%,while synaptic gephyrin S270 phosphorylation increased by 18.3% in DZP-treated neurons after 24 h compared to control(P<0.05).Dendritic levels of gephyrin were also reduced to 74.1% of control,while S270 phosphorylation was elevated by 25.2%(P<0.05;P<0.01).Mice 12 h post-DZP injection demonstrated a 12.7% and 26.1% decrease in total γ2 and gephyrin levels,respectively(P<0.05;P<0.01).12 h DZP treatment enhanced γ2 subunit ubiquitination 1.13-fold relative to control(P<0.05).Internalized γ2 pH FAP GABA A Rs associated with lysosomes was 8.0% higher in neurons treated with 12-16 h DZP compared to control.Pilot FRAP experiments suggest gephyrin and γ2 have increased mobility and turnover at synapses following DZP.CONCLUSION DZP treatment decreases γ2 GABA A R levels and gephyrin scaffolding function after one day of exposure,which may contribute to the formation of DZP tolerance. 展开更多
关键词 gaba type A receptor GEPHYRIN TRAFFICKING DIAZEPAM
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Effects of Nourishing “Yin”-Removing “Fire” Chinese Herb Mixture on the Differential Expression of GABA<sub>A</sub>Receptor <i>α</i>Subunits in Hypothalamus of Precocious Puberty Female Rats
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作者 Jing Li Yanyan Sun +2 位作者 Shiran Wang Jian Yu Zhanzhuang Tian 《Chinese Medicine》 2013年第3期87-96,共10页
GABAergic input to Gonadotropin-releasing hormone (GnRH) neurons is necessary to initiate the onset of puberty and its action mainly depends on GABAA receptor of which the subunit composition, properties and consequen... GABAergic input to Gonadotropin-releasing hormone (GnRH) neurons is necessary to initiate the onset of puberty and its action mainly depends on GABAA receptor of which the subunit composition, properties and consequently function varies during this period. Nourishing “Yin”-Removing “Fire” Chinese herb mixture, a Chinese herb-based formulation, has been proved that it may retard the initiation of pubertal development in female precocious puberty rats. Our objective is to investigate the effects of Nourishing “Yin”-Removing “Fire” Chinese herb mixture on the expression of GABAA receptor α subunits in hypothalamus. Female Sprague-Dawley rats were divided into normal (N), precocious puberty model (M) induced by danazol, model exposed to saline (MS) and model exposed to Chinese herb mixture (CHM) groups. All rats were administered by the Chinese herb mixture from P15 on. Coefficients of reproductive organs and serum gonadotropins and estradiol levels in M were significantly enhanced while they were significantly decreased in CHM. The hypothalamic GnRH mRNA was also significantly increased in M and in CHM, as well as ERα mRNA. At the mean time, the hypothalamic GABAA receptor α1 and α3 subunits mRNA were more significantly decreased in M than those of N, while they were more significantly enhanced in CHM than those in M (p 0.01), the protein expression of which in hypothalamus had the same trend as the mRNA expression. The evidence suggests that Nourishing “Yin”-Removing “Fire” Chinese herb mixture could significantly retard the sexual development of the precocious rats, and up-regulate the expressions of hypothalamic GABAA receptor α1 and α3 subunits. Our result indicated that GABAA receptor α1 and α3 subunits might involve in the effective treatment of herb mixture on idiopathic precocious puberty. 展开更多
关键词 gaba gabaA receptor α Subunit PRECOCIOUS Puberty Nourishing “Yin”-Removing “Fire” Chinese Herb MIXTURE Rat
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Differential Effect of Unilateral Amygdalar GABAA Receptor Agonist Injection on Low- and High-Anxiety Rats
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作者 Maria P. Rysakova Irina V. Pavlova 《Journal of Behavioral and Brain Science》 2016年第1期9-18,共10页
The influence of γ-aminobutyric type-A (GABA<sub>A</sub>) receptors agonist (muscimol hydrobromide, 0.1 μg/0.5 μl) injections into the right or left basolateral amygdala (BLA) on the behavior of high-an... The influence of γ-aminobutyric type-A (GABA<sub>A</sub>) receptors agonist (muscimol hydrobromide, 0.1 μg/0.5 μl) injections into the right or left basolateral amygdala (BLA) on the behavior of high-anxiety (HA) and low-anxiety (LA) rats subjected to the elevated plus-maze (EPM) test was investigated. Anxiolytic-like effects (increase of open-arm entries and open-arm time) was revealed only after administration of muscimol into the left (but not right) amygdala of HA animals. No effect was observed upon administration of muscimol to LA rats. These findings suggest an important role in anxiety regulation of the amygdalar GABA levels, and the assumed GABA hemispheric lateralization. 展开更多
关键词 ANXIETY Basolateral Amygdala gabaA receptor Muscimol Hydrobromide Hemispheric Lateralization
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表皮穿透和GABA_A受体不敏感性在小菜蛾对阿维菌素抗性中的作用 被引量:25
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作者 吴青君 张文吉 +2 位作者 张友军 徐宝云 朱国仁 《昆虫学报》 CAS CSCD 北大核心 2002年第3期336-340,共5页
用氚标记阿维菌素点滴处理阿维菌素敏感 (ABM S)和抗性 (ABM R)种群小菜蛾幼虫 ,结果显示 ,在 5~ 36 0min内的 7个不同处理时间 ,ABM R种群的平均表皮穿透量比ABM S种群少 1 5倍 ,处理 2 4h后 ,ABM R种群仍有 45 9%的3 H 阿维菌素滞... 用氚标记阿维菌素点滴处理阿维菌素敏感 (ABM S)和抗性 (ABM R)种群小菜蛾幼虫 ,结果显示 ,在 5~ 36 0min内的 7个不同处理时间 ,ABM R种群的平均表皮穿透量比ABM S种群少 1 5倍 ,处理 2 4h后 ,ABM R种群仍有 45 9%的3 H 阿维菌素滞留于体表 ,而ABM S种群却有 98 4%的药剂穿透表皮。放射配体结合分析表明 ,GABAA 受体结合性质的改变是小菜蛾对阿维菌素的另一抗性机制 ,ABM S种群 (Kd=10 936 8± 0 4374nmol L)和ABM R种群 (Kd=9 832 8± 0 3933nmol L)的受体亲和力无显著差异 ,但抗性种群的最大结合量 (Bmax =71 2 842± 4 9910fmol mg蛋白 )比敏感种群 (Bmax =112 0 2 5 5± 7 8418fmol mg蛋白 )降低 6 3 6 % ,即抗性是受体数目的减少而非结构上的改变。 展开更多
关键词 小菜蛾 阿维菌素 抗药性 表皮穿透作用 gabaA 受体
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激活GABA_B受体在针刺镇痛中的作用 被引量:21
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作者 朱丽霞 叶燕燕 +1 位作者 莫孝荣 吉长福 《针刺研究》 CAS CSCD 2002年第2期85-91,共7页
目的 :脑室注射γ 氨基丁酸 (GABA)A受体的拮抗剂荷包牡丹碱 (Bic)未能阻断针刺镇痛效应 ,微电泳导入Bic部分阻断电针抑制脊髓背角伤害性反应 ,说明GABA可通过激活A受体参与针刺镇痛中脊髓节段性抑制。本文进一步探讨了激活GABAB 受体... 目的 :脑室注射γ 氨基丁酸 (GABA)A受体的拮抗剂荷包牡丹碱 (Bic)未能阻断针刺镇痛效应 ,微电泳导入Bic部分阻断电针抑制脊髓背角伤害性反应 ,说明GABA可通过激活A受体参与针刺镇痛中脊髓节段性抑制。本文进一步探讨了激活GABAB 受体在针刺镇痛中的作用。方法 :以辐射热照射大鼠尾部引起甩尾反射潜伏期作为痛阈的指标 ,以针刺“次”穴后痛阈最大变化百分率判断镇痛效应 ,观察脑室注射 (icv) 5μL或蛛网膜下腔 (ith)注射 1 0 μLGABAB 受体的拮抗剂CGP 55845对针刺镇痛效应的影响。每组 6~ 8例。结果 :icvGABA( 1 2 5μg、2 50 μg、50 0 μg)或GABAB 受体激动剂苯氯丁氨酸 (Baclofen ,2 5ng、2 50ng、2 50 0ng)可产生剂量依赖的镇痛效应。icvCGP 55845( 5ng、50ng)可大部分阻断GABA和Baclofen的镇痛效应。针刺双侧“次”穴( 50Hz,1~ 2mA) 1 0min ,痛阈提高到针前值的 ( 1 42 .5± 2 .1 ) % ,镇痛效应显著。针前icvCGP55845针后痛阈分别提高到 ( 1 1 1 .2± 1 .2 ) %和 ( 1 1 2 .1± 1 .1 ) % ,阻断率分别为 73 .7%和 71 .6% ,和事先icv生理盐水 ( 1 43 .7± 2 .0 ) %相比 ,阻断效应明显。若针刺前ithCGP 55845( 50ng、50 0ng) ,也能明显阻断针刺镇痛效应。结论 :脑内注射GABA或Baclofen可通过激? 展开更多
关键词 gabaB受体激动剂 BACLOFEN gabaB受体拮抗剂 CGP 55845 针刺镇痛
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盐酸川芎嗪通过干预GABAR和FOXP2的表达保护低压低氧大鼠学习记忆 被引量:13
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作者 李晓娜 汪晓筠 +5 位作者 朱艳媚 曹成珠 杨春燕 严云飞 赵延礼 李生花 《中国药理学通报》 CAS CSCD 北大核心 2017年第9期1285-1290,共6页
目的探讨盐酸川芎嗪对低压低氧大鼠学习记忆功能的影响及其作用机制。方法将120只SD大鼠随机分为2组,低氧对照组(5 500 m)、低氧药物组(5 500 m),按时间段不同又分为1 d、3 d、7 d、15 d、30 d组,每组12只;对照组和药物组在模拟海拔550... 目的探讨盐酸川芎嗪对低压低氧大鼠学习记忆功能的影响及其作用机制。方法将120只SD大鼠随机分为2组,低氧对照组(5 500 m)、低氧药物组(5 500 m),按时间段不同又分为1 d、3 d、7 d、15 d、30 d组,每组12只;对照组和药物组在模拟海拔5500 m的低压氧仓造模,对照组腹腔注射生理盐水,药物组用同样的方法注射盐酸川芎嗪进行干预。用Morris水迷宫实验检测大鼠行为学变化;Western blot检测大鼠海马GABAAα1R、GABAB1R、FOXP2表达情况。结果(1)通过计算对照组和药物组定位航行实验中的总路程和穿越平台次数可以得出,两组1 d结果差异无统计学意义(P>0.05),从3 d组开始,药物组总路程较对照组逐渐缩短(P<0.01),而穿越中心平台次数较对照组逐渐增多(P<0.01);(2)Western blot检测海马GABAAα1R受体,不同时间段对照组与药物组海马中该受体表达差异无统计学意义(P>0.05);GABAB1R受体和FOXP2蛋白,1 d对照组药物组表达没有差异,从3 d组开始,对照组该受体和蛋白表达量均低于药物组(P<0.05);(3)对照组海马中GABAB1R与水迷宫总路程呈负相关(r=-0.738,P<0.05);对照组海马中FOXP2蛋白与水迷宫总路程呈负相关(r=-0.693,P<0.05);对照组海马中GABAB1R、FOXP2蛋白表达呈正相关(r=0.834,P<0.05)。结论盐酸川芎嗪对低压低氧大脑学习记忆能力起到一定的保护作用,其机制可能与增加大鼠脑内递质GABAB1R和蛋白FOXP2表达量有关。 展开更多
关键词 盐酸川芎嗪 低压低氧 海马 水迷宫 学习记忆 gabaR FOXP2
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调理心肾中药对拟痴呆大鼠脑组织中M和GABA受体功能的影响 被引量:10
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作者 莫启忠 宫斌 +5 位作者 陈坤华 方军 李伟雄 王菊美 匡兴伟 陈荣 《核技术》 CAS CSCD 北大核心 1993年第5期295-298,共4页
以~3H-QNB和~3H-GABA为放射性配基,用受体放射性配基结合分析法,测出拟痴呆模型大鼠大脑皮层和海马组织中的M受体和小脑组织中的GABA受体的R_t值明显降低;M受体的K_D值在大脑皮层中明显减少,在海马中略有升高。小脑中GABA受体的K_D值显... 以~3H-QNB和~3H-GABA为放射性配基,用受体放射性配基结合分析法,测出拟痴呆模型大鼠大脑皮层和海马组织中的M受体和小脑组织中的GABA受体的R_t值明显降低;M受体的K_D值在大脑皮层中明显减少,在海马中略有升高。小脑中GABA受体的K_D值显著降低。调理心肾中药及喜德镇(Hydergin,为国外常用抗老年痴呆药)能使降低的M受体和GABA受体的R_t值均明显升高,接近正常水平。对K_D值则有不同程度的调整作用。 展开更多
关键词 胆碱能 衰茏 Γ氨基丁酸 心肾不交
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羟丁酸钠对大鼠原代培养皮层神经元缺氧复氧损伤的保护作用与GABA_A受体的关系 被引量:10
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作者 谷淑玲 李梅 +2 位作者 崔家勇 姚兵 戴体俊 《中国临床药理学与治疗学》 CAS CSCD 2002年第5期385-388,共4页
目的 :探讨羟丁酸钠 (SO)对大鼠皮层神经元缺氧复氧损伤的保护作用与GABAA 受体的关系。方法 :采用原代培养大鼠皮层神经元建立缺氧复氧损伤模型 ,观察细胞的形态学 ,测定其LDH漏出率、MDA含量、SOD、GPx活力。结果 :缺氧复氧可引起神... 目的 :探讨羟丁酸钠 (SO)对大鼠皮层神经元缺氧复氧损伤的保护作用与GABAA 受体的关系。方法 :采用原代培养大鼠皮层神经元建立缺氧复氧损伤模型 ,观察细胞的形态学 ,测定其LDH漏出率、MDA含量、SOD、GPx活力。结果 :缺氧复氧可引起神经元损伤 ,LDH漏出率增加 ,MDA含量升高 (P <0 .0 1) ,SOD、GPx活力降低 (P <0 .0 1)。SO能显著减少损伤神经元的LDH漏出率及MDA的生成 (P <0 .0 1) ,升高SOD、GPx(P <0 .0 1)的活力 ,这种作用可被GABAA 受体阻断剂seurinine减弱 (P <0 .0 1)。结论 :SO对缺氧复氧神经元损伤的保护作用可能与其激动GABAA 受体有关。 展开更多
关键词 羟丁酸钠 gabaA受体 缺氧复氧损伤 脑缺血 血脑屏障
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有机磷农药急性中毒对大鼠GABA受体影响的研究 被引量:6
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作者 彭俊华 张峰 +3 位作者 齐心亮 曹波 高宁 卓鉴波 《中国现代医学杂志》 CAS CSCD 2000年第5期13-14,共2页
探索有机磷农药急性中毒的γ -氨基丁酸系统机理 ,为有机磷农药急性中毒的治疗提供理论依据。实验 :用大鼠脑神经末梢微囊GABA受体做模型 ,从大鼠体外实验、体内染毒实验 (动物抽搐发作和不发作 ) ,观察GABA受体的变化。结果 :在体外实... 探索有机磷农药急性中毒的γ -氨基丁酸系统机理 ,为有机磷农药急性中毒的治疗提供理论依据。实验 :用大鼠脑神经末梢微囊GABA受体做模型 ,从大鼠体外实验、体内染毒实验 (动物抽搐发作和不发作 ) ,观察GABA受体的变化。结果 :在体外实验中 ,1× 10 -2 mol/L的二嗪农或丙氟磷能显著降低大鼠GABA受体的结合 (P <0 .0 1) ,1× 10 -3 mol/L的二嗪农仍能显著降低GABA受体的结合 (P <0 .0 5 )。二嗪农 1.0 95 g/kg灌胃大鼠 ,结果发现3 H -GABA的结合值在抽搐发作时显著降低 ,大鼠腹腔注射丙氟磷 6mg/kg ,观察大鼠抽搐发作与不发作 ,3 H -GABA的结合值均显著降低。结论 :有机磷农药在一定浓度下能显著降低大鼠脑GABA受体的结合 。 展开更多
关键词 有机磷农药 受体 gaba受体 中毒
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周边γ-氨基丁酸通过GABA_B受体调控骶髓后联合核神经元谷氨酸能突触 被引量:5
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作者 马红雨 林凯 +2 位作者 罗丹 吕建晓 杨鲲 《中国药理学通报》 CAS CSCD 北大核心 2011年第9期1231-1235,共5页
目的研究突触周边γ-氨基丁酸(ambient GABA)通过GABAB受体调控骶髓后联合核(SDCN)神经元谷氨酸能突触的机制。方法在急性切取的骶段脊髓薄片上,利用全细胞膜片钳法记录骶髓后联合核神经元谷氨酸能兴奋性突触后电流(EPSCs),将GABAB受体... 目的研究突触周边γ-氨基丁酸(ambient GABA)通过GABAB受体调控骶髓后联合核(SDCN)神经元谷氨酸能突触的机制。方法在急性切取的骶段脊髓薄片上,利用全细胞膜片钳法记录骶髓后联合核神经元谷氨酸能兴奋性突触后电流(EPSCs),将GABAB受体用其特异性受体拮抗剂CGP52432阻断,观察谷氨酸突触终末上的GABAB受体被周边GABA作用的影响。结果在突触后GABAB受体被从胞内阻断的条件下,再灌流CGP52432阻断谷氨酸能突触前GABAB受体,可增加刺激引发的EPSCs(eEPSCs)幅度;改变配对刺激的两个EPSC比率(paired-pulse ratio,PPR),并激发沉默突触(silent synapse)。但CGP52432对微小兴奋性突触后电流(mEPSCs)无影响。结论位于SDCN神经元谷氨酸能突触前的GABAB受体受周边GABA调控。这种影响参与调节谷氨酸释放并可能参与痛觉信息在脊髓水平的传递。 展开更多
关键词 骶髓后联合核 Γ-氨基丁酸 gabaB受体 谷氨酸 全细胞记录 脊髓 大鼠
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UDMH对GABA及其受体影响的研究 被引量:4
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作者 彭俊华 曹波 +3 位作者 高宁 龙冬梅 张峰 齐心亮 《中国现代医学杂志》 CAS CSCD 2001年第6期8-9,共2页
目的 :探索UDMH急性中毒的γ -氨基丁酸及其受体机制 ,为UDMH急性中毒的治疗提供论理依据。实验 :大鼠气管染毒 ,测定脑组织中GABA含量和GAD活性 ,观察脑神经末梢微囊受体的变化。结果 :UDMH使脑组织中GABA含量和GAD活力显著降低 (P <... 目的 :探索UDMH急性中毒的γ -氨基丁酸及其受体机制 ,为UDMH急性中毒的治疗提供论理依据。实验 :大鼠气管染毒 ,测定脑组织中GABA含量和GAD活性 ,观察脑神经末梢微囊受体的变化。结果 :UDMH使脑组织中GABA含量和GAD活力显著降低 (P <0 .0 1)。体外试验发现UDMH使GABA与其受体的结合下降 ;体内染毒试验发现在大鼠惊厥发作前GABA受体的结合显著下降 ,惊厥发作时GABA与受体的结合显著上升。结论 展开更多
关键词 偏二甲基肼 Γ-氨基丁酸 谷氨酸脱羧酶 Γ-氨基丁酸受体 中毒
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Mg^(2+)对神经元保护机制的研究-Mg^(2+)对培养的大鼠海马神经元GABA_A受体介导电流的影响 被引量:3
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作者 邓学军 胡波 +2 位作者 梅元武 孙圣刚 童萼塘 《中风与神经疾病杂志》 CAS CSCD 北大核心 2002年第6期326-328,共3页
目的 研究镁离子(Mg2+)对神经元保护的机制。方法 采用全细胞膜片钳技术,研究Mg2+对培养的大鼠海马神经元GABA_A受体介导电流的作用。结果 (1)在钳制电压为-40mV时,GABA可通过GABA_A受体介导产生内向电流;(2)当GABA和Mg2+同时作用时,该... 目的 研究镁离子(Mg2+)对神经元保护的机制。方法 采用全细胞膜片钳技术,研究Mg2+对培养的大鼠海马神经元GABA_A受体介导电流的作用。结果 (1)在钳制电压为-40mV时,GABA可通过GABA_A受体介导产生内向电流;(2)当GABA和Mg2+同时作用时,该电流峰值增高;(3)在Mg2+存在的情况下,GABA的浓度-效应曲线平行左移。结论 Mg2+通过正性变构调节机制影响GABA_A受体的功能,达到保护神经元的作用。 展开更多
关键词 神经元保护 海马 MG^2+ gabaA受体 全细胞记录 全细胞膜片钳技术
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黄芩茎叶黄酮作为GABA_A受体BZD结合部位配体(英文) 被引量:9
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作者 王红燕 韩敬贤 +3 位作者 徐绥绪 陈英杰 王子晖 薛红 《中国药物化学杂志》 CAS CSCD 2002年第5期265-267,共3页
目的从黄芩地上部分中寻找活性成分。方法利用各种柱色谱 (硅胶、SephadexLH 2 0、D10 1大孔吸附树脂和聚酰胺 )分离黄芩地上部分的活性成分。结果从黄芩地上部分的水提取物中分离得到 7种黄酮类化合物。其中白杨素对GABAA 受体的BZD结... 目的从黄芩地上部分中寻找活性成分。方法利用各种柱色谱 (硅胶、SephadexLH 2 0、D10 1大孔吸附树脂和聚酰胺 )分离黄芩地上部分的活性成分。结果从黄芩地上部分的水提取物中分离得到 7种黄酮类化合物。其中白杨素对GABAA 受体的BZD结合部位有较高的亲和力 ,其IC50 值为 0 6 7μmol/L。 7种黄酮类化合物亲和力的排列顺序为 :白杨素 >汉黄芩苷元 >红花素 >黄芩素 >5 ,6 ,7 三羟基 4′ 甲氧基黄酮 >异红花素 >白杨素 7 葡萄糖醛酸苷。 展开更多
关键词 黄芩茎叶黄酮 gabaA受体 BZD结合部位 黄芩 水提取物 分离
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急性热应激对小鼠大脑皮质GABA受体的影响 被引量:12
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作者 陈忠 李书珍 朱剑琴 《南京大学学报(自然科学版)》 CAS CSCD 1997年第3期386-391,共6页
用放射配体结合分析方法和小鼠经受急性热应激致肛温达42℃时的热应激模型,研究了小鼠大脑皮层中两类GABA受体亚型(GABAA受体和GABAB受体)结合能力变化,以及氯丙嗪对GABA受体的影响.通过Scatchard作... 用放射配体结合分析方法和小鼠经受急性热应激致肛温达42℃时的热应激模型,研究了小鼠大脑皮层中两类GABA受体亚型(GABAA受体和GABAB受体)结合能力变化,以及氯丙嗪对GABA受体的影响.通过Scatchard作图分析表明:1)急性热应激组小鼠大脑皮层GABAA受体Bmax值明显上调,而GABAB受体Bmax值则明显下调;2)氯丙嗪组小鼠大脑皮层GABAA受体增多出现上调现象,而GABAB受体则为下调;3)氯丙嗪热应激组小鼠大脑皮层的两类受体增多出现上调现象,且肛温明显低于42℃.这些结果揭示:GABA受体可能参予了热应激的调节过程,且两类不同受体有不同的作用方式,氯丙嗪也可能通过GABA受体的介导,在改善热应激损伤中起主要作用. 展开更多
关键词 急性热应激 gaba受体 氯丙嗪 大脑皮质 热应激
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