• 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

大鼠纹状体突触膜的腺苷酸环化酶活性。毒蕈碱受体激动剂的抑制作用。

Adenylate cyclase activity of synaptic membranes from rat striatum. Inhibition by muscarinic receptor agonists.

作者信息

Olianas M C, Onali P, Neff N H, Costa E

出版信息

Mol Pharmacol. 1983 Mar;23(2):393-8.

PMID:6188035
Abstract

Acetylcholine inhibits, by 30-40%, the basal adenylate cyclase activity of purified synaptic plasma membranes prepared from rat striatum (EC50 = 3 microM). Cholinergic receptor agonists inhibit this cyclase activity with the following rank order of potency: oxtremorine greater than acetylcholine greater than arecoline greater than methacholine greater than or equal to muscarine greater than or equal to carbachol greater than bethanechol. Nicotine fails to inhibit the cyclase, and d-tubocurarine fails to inhibit the action of cholinergic drugs. In contrast, atropine and scopolamine antagonize the effect of acetylcholine. The enzyme inhibition elicited by acetylcholine requires the presence of GTP, and disappears after intrastriatal injection of kainic acid. From these results, we infer that striatal adenylate cyclase can be modulated by muscarinic receptors.

摘要

乙酰胆碱可使从大鼠纹状体制备的纯化突触质膜的基础腺苷酸环化酶活性抑制30%-40%(半数有效浓度EC50 = 3微摩尔)。胆碱能受体激动剂抑制该环化酶活性的效力顺序如下:震颤素>乙酰胆碱>槟榔碱>醋甲胆碱≥毒蕈碱≥卡巴胆碱>氨甲酰甲胆碱。尼古丁不能抑制该环化酶,筒箭毒碱也不能抑制胆碱能药物的作用。相反,阿托品和东莨菪碱可拮抗乙酰胆碱的作用。乙酰胆碱引起的酶抑制作用需要鸟苷三磷酸(GTP)的存在,且在纹状体内注射 kainic 酸后消失。从这些结果我们推断,纹状体腺苷酸环化酶可受毒蕈碱受体调节。

相似文献

1
Adenylate cyclase activity of synaptic membranes from rat striatum. Inhibition by muscarinic receptor agonists.大鼠纹状体突触膜的腺苷酸环化酶活性。毒蕈碱受体激动剂的抑制作用。
Mol Pharmacol. 1983 Mar;23(2):393-8.
2
Characterization of dopamine receptors mediating inhibition of adenylate cyclase activity in rat striatum.介导大鼠纹状体腺苷酸环化酶活性抑制的多巴胺受体的特性分析。
Mol Pharmacol. 1985 Aug;28(2):138-45.
3
Effects of clozapine on rat striatal muscarinic receptors coupled to inhibition of adenylyl cyclase activity and on the human cloned m4 receptor.氯氮平对与腺苷酸环化酶活性抑制偶联的大鼠纹状体毒蕈碱受体及对人克隆M4受体的作用。
Br J Pharmacol. 1997 Oct;122(3):401-8. doi: 10.1038/sj.bjp.0701357.
4
Muscarinic stimulation of adenylate cyclase activity of rat olfactory bulb. II. Characterization of the antagonist sensitivity and comparison with muscarinic inhibitions of the enzyme in striatum and heart.毒蕈碱对大鼠嗅球腺苷酸环化酶活性的刺激作用。II. 拮抗剂敏感性的特征及与纹状体和心脏中该酶的毒蕈碱抑制作用的比较。
J Pharmacol Exp Ther. 1991 Nov;259(2):680-6.
5
Muscarinic receptor regulation of NG108-15 adenylate cyclase: requirement for Na+ and GTP.毒蕈碱受体对NG108 - 15腺苷酸环化酶的调节:对钠离子和鸟苷三磷酸的需求
J Cyclic Nucleotide Res. 1979 Oct;5(5):367-75.
6
Muscarinic receptor-mediated phosphoinositide hydrolysis in the rat retina.毒蕈碱受体介导的大鼠视网膜磷酸肌醇水解作用
J Pharmacol Exp Ther. 1988 Aug;246(2):553-7.
7
Identification and characterization of muscarinic receptors potentiating the stimulation of adenylyl cyclase activity by corticotropin-releasing hormone in membranes of rat frontal cortex.大鼠额叶皮质膜中增强促肾上腺皮质激素释放激素对腺苷酸环化酶活性刺激作用的毒蕈碱受体的鉴定与表征
J Pharmacol Exp Ther. 1998 Aug;286(2):753-9.
8
Muscarinic acetylcholine receptors linked to the inhibition of adenylate cyclase activity in membranes from the rat striatum and myocardium can be distinguished on the basis of agonist efficacy.与大鼠纹状体和心肌细胞膜中腺苷酸环化酶活性抑制相关的毒蕈碱型乙酰胆碱受体可根据激动剂效力加以区分。
Mol Pharmacol. 1988 Dec;34(6):769-78.
9
Guanine nucleotide binding sites, responsible for adenylate cyclase activation and carbamylcholine binding inhibition, show similar properties in rat heart membranes.负责激活腺苷酸环化酶和抑制氨甲酰胆碱结合的鸟嘌呤核苷酸结合位点,在大鼠心脏膜中表现出相似的特性。
J Cyclic Nucleotide Res. 1981;7(3):173-85.
10
A comparison of the regulatory properties of striatal and cortical adenylate cyclase.纹状体和皮质腺苷酸环化酶调节特性的比较。
Neurobiol Aging. 1993 Jan-Feb;14(1):65-72. doi: 10.1016/0197-4580(93)90024-6.

引用本文的文献

1
Muscarinic inhibition of hippocampal and striatal adenylyl cyclase is mainly due to the M(4) receptor.毒蕈碱对海马体和纹状体腺苷酸环化酶的抑制作用主要归因于M(4)受体。
Neurochem Res. 2009 Aug;34(8):1363-71. doi: 10.1007/s11064-009-9916-9. Epub 2009 Feb 4.
2
Rat striatal muscarinic receptors coupled to the inhibition of adenylyl cyclase activity: potent block by the selective m4 ligand muscarinic toxin 3 (MT3).与腺苷酸环化酶活性抑制相关联的大鼠纹状体毒蕈碱受体:选择性M4配体毒蕈碱毒素3(MT3)的强效阻断作用。
Br J Pharmacol. 1996 May;118(2):283-8. doi: 10.1111/j.1476-5381.1996.tb15400.x.
3
Antagonism by (R)- and (S)-trihexyphenidyl of muscarinic stimulation of adenylyl cyclase in rat olfactory bulb and inhibition in striatum and heart.
(R)-和(S)-苯海索对大鼠嗅球中毒蕈碱刺激腺苷酸环化酶以及对纹状体和心脏中该酶抑制作用的拮抗效应
Br J Pharmacol. 1994 Nov;113(3):775-80. doi: 10.1111/j.1476-5381.1994.tb17060.x.
4
Acceleration of desipramine-induced changes on the dopamine receptor-coupled adenylate cyclase system by pertussis toxin.百日咳毒素加速地昔帕明对多巴胺受体偶联腺苷酸环化酶系统的影响
J Neural Transm Gen Sect. 1994;98(2):133-42. doi: 10.1007/BF01277016.
5
Affinities of muscarinic drugs for [3H]N-methylscopolamine (NMS) and [3H]oxotremorine (OXO) binding to a mixture of M1-M4 muscarinic receptors: use of NMS/OXO-M ratios to group compounds into potential agonist, partial agonist, and antagonist classes.毒蕈碱类药物与[3H]N-甲基东莨菪碱(NMS)及[3H]震颤素(OXO)结合至M1 - M4毒蕈碱受体混合物的亲和力:利用NMS/OXO - M比率将化合物分为潜在激动剂、部分激动剂和拮抗剂类别。
Neurochem Res. 1995 Jun;20(6):669-74. doi: 10.1007/BF01705534.
6
Pertussis vaccine reduces agonist binding to the rat heart muscarinic receptor and its guanine nucleotide modulation.百日咳疫苗可降低激动剂与大鼠心脏毒蕈碱受体的结合及其鸟嘌呤核苷酸调节作用。
Neurochem Res. 1986 May;11(5):745-52. doi: 10.1007/BF00965342.
7
Atrial muscarinic receptors: effect of Triton X-100 on guanine nucleotide and ammonium ion modulation.心房毒蕈碱受体:曲拉通X-100对鸟嘌呤核苷酸和铵离子调节的影响
Neurochem Res. 1986 Mar;11(3):437-51. doi: 10.1007/BF00965017.
8
Reconstitution of solubilized atrial cholinergic muscarinic receptors in liposomes.脂质体中溶解的心房胆碱能毒蕈碱受体的重组。
Neurochem Res. 1987 Jan;12(1):83-91. doi: 10.1007/BF00971369.
9
Relative affinities of drugs acting at cholinoceptors in displacing agonist and antagonist radioligands: the NMS/Oxo-M ratio as an index of efficacy at cortical muscarinic receptors.作用于胆碱能受体的药物在置换激动剂和拮抗剂放射性配体方面的相对亲和力:NMS/Oxo-M 比值作为皮质毒蕈碱受体效能的指标。
Br J Pharmacol. 1988 Feb;93(2):437-45. doi: 10.1111/j.1476-5381.1988.tb11451.x.
10
Effects of oxotremorine and RMI 12330 A on [3H]acetylcholine release and adenylate cyclase activity in guinea pig superior cervical ganglion.氧化震颤素和RMI 12330 A对豚鼠颈上神经节中[3H]乙酰胆碱释放及腺苷酸环化酶活性的影响。
Neurochem Res. 1988 Nov;13(11):1049-53. doi: 10.1007/BF00973149.