• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

果蝇中枢神经系统膜中[(3)H]γ-氨基丁酸结合位点的表征

Characterization of binding sites for [(3)H]Gaba in Drosophila melanogaster CNS membranes.

作者信息

Rosario P, Barat A, Ramirez G

机构信息

Centro de Biologia Molecular, CSIC-UAM, Cantoblanco, 28049 Madrid, Spain.

出版信息

Neurochem Int. 1989;15(1):115-20. doi: 10.1016/0197-0186(89)90083-1.

DOI:10.1016/0197-0186(89)90083-1
PMID:20504472
Abstract

Drosophila melanogaster membranes prepared from cephalic ganglia contain two apparently independent populations of saturable binding sites for [(3)H]GABA: the higher-affinity sites (K(d) = 23 nM; B(max = 0.97 pmol/mg)) are already labeled at 0 degrees C, while a lower-affinity population of binding sites (K(d = 258 nM); B(max = 8.51 pmol/mg)) can be additionally identified at 23 degrees C and higher temperatures. GABA and then muscimol, together with ?-aminovalerate, are very efficient displacers of the specific binding while the A-specific agonist isoguvacine, the A-specific antagonist bicuculline methiodide and the B-specific agonist baclofen have low to negligible effect. [(3)H]GABA binding is not modulated by allosteric effectors characteristic of the vertebrate A-site, except for an anomalous stimulation by DMCM. Both [(3)H]flunitrazepam and [(3)H]TBOB give "specific" binding values under different experimental conditions but, after kinetic analysis, the binding appears to be non-saturable in both cases. We conclude that there are marked differences between the Drosophila GABA receptor and the vertebrate GABA(A) receptor complex, although our results do not exclude the existence of an insect receptor complex, associated to a Cl(?) channel, with different structural and pharmacological properties.

摘要

从头部神经节制备的黑腹果蝇膜含有两类明显独立的可饱和[³H]GABA结合位点:高亲和力位点(Kd = 23 nM;Bmax = 0.97 pmol/mg)在0℃时就已被标记,而低亲和力结合位点群体(Kd = 258 nM;Bmax = 8.51 pmol/mg)在23℃及更高温度下可额外鉴定出来。GABA以及随后的蝇蕈醇,连同γ-氨基戊酸,是特异性结合的非常有效的置换剂,而A特异性激动剂异鹅膏蕈氨酸、A特异性拮抗剂荷包牡丹碱甲碘化物和B特异性激动剂巴氯芬的作用很低或可忽略不计。除了被DMCM异常刺激外,[³H]GABA结合不受脊椎动物A位点特征性变构效应剂的调节。[³H]氟硝西泮和[³H]TBOB在不同实验条件下都给出“特异性”结合值,但经过动力学分析后,两种情况下的结合似乎都是不饱和的。我们得出结论,果蝇GABA受体与脊椎动物GABA(A)受体复合物之间存在显著差异,尽管我们的结果不排除存在与氯离子通道相关的具有不同结构和药理学特性的昆虫受体复合物。

相似文献

1
Characterization of binding sites for [(3)H]Gaba in Drosophila melanogaster CNS membranes.果蝇中枢神经系统膜中[(3)H]γ-氨基丁酸结合位点的表征
Neurochem Int. 1989;15(1):115-20. doi: 10.1016/0197-0186(89)90083-1.
2
The GABA(A) receptor complex in the developing chick optic tectum: characterization of [(3)H]muscimol binding sites.发育中的雏鸡视顶盖中的GABA(A)受体复合物:[³H]蝇蕈醇结合位点的特性
Neurochem Int. 1987;10(4):405-11. doi: 10.1016/0197-0186(87)90066-0.
3
Binding sites for [(3)H]GABA, [(3)H]flunitrazepam and [(35)S]TBPS in insect CNS.昆虫中枢神经系统中[(3)H]γ-氨基丁酸、[(3)H]氟硝西泮和[(35)S]叔丁基双环磷硫酰胺的结合位点
Neurochem Int. 1986;9(2):287-93. doi: 10.1016/0197-0186(86)90065-3.
4
Characterization of the GABA(A) receptor in the brain of the adult male bullfrog, Rana catesbeiana.成年雄性牛蛙(牛蛙)大脑中GABA(A)受体的特征
Brain Res. 2003 Nov 28;992(1):69-75. doi: 10.1016/j.brainres.2003.08.030.
5
Modulation of GABA binding sites by CNS depressants and CNS convulsants.中枢神经系统抑制剂和中枢神经系统惊厥剂对γ-氨基丁酸(GABA)结合位点的调节作用。
Neurochem Int. 1982;4(4):259-68. doi: 10.1016/0197-0186(82)90062-6.
6
Bicuculline-insensitive GABA binding to catfish neuronal membranes.荷包牡丹碱不敏感的γ-氨基丁酸与鲶鱼神经元膜的结合
Neurochem Int. 1988;12(2):125-9. doi: 10.1016/0197-0186(88)90119-2.
7
Characteristics of GABAB receptor binding sites on rat whole brain synaptic membranes.大鼠全脑突触膜上GABAB受体结合位点的特征
Br J Pharmacol. 1983 Jan;78(1):191-206. doi: 10.1111/j.1476-5381.1983.tb09380.x.
8
Allosteric uncoupling and up-regulation of benzodiazepine and GABA recognition sites following chronic diazepam treatment of HEK 293 cells stably transfected with alpha1beta2gamma2S subunits of GABA (A) receptors.在用GABA(A)受体的α1β2γ2S亚基稳定转染的HEK 293细胞中,长期给予地西泮治疗后,苯二氮䓬和GABA识别位点的变构解偶联及上调。
Naunyn Schmiedebergs Arch Pharmacol. 2007 May;375(3):177-87. doi: 10.1007/s00210-007-0152-z. Epub 2007 Mar 22.
9
Characterization of [3H]thiocolchicoside binding sites in rat spinal cord and cerebral cortex.大鼠脊髓和大脑皮层中[3H]硫代秋水仙碱结合位点的表征
Eur J Pharmacol. 1999 Jul 2;376(1-2):149-57. doi: 10.1016/s0014-2999(99)00371-4.
10
Honokiol and magnolol increase the number of [3H] muscimol binding sites three-fold in rat forebrain membranes in vitro using a filtration assay, by allosterically increasing the affinities of low-affinity sites.厚朴酚与和厚朴酚在体外利用过滤分析法使大鼠前脑细胞膜中[3H]蝇蕈醇结合位点的数量增加了两倍,这是通过变构增加低亲和力位点的亲和力实现的。
Neurochem Res. 1999 Dec;24(12):1593-602. doi: 10.1023/a:1021116502548.