喹诺酮类抗菌剂对γ-氨基丁酸与大鼠脑膜受体位点结合的抑制作用。
Inhibitory effects of quinolone antibacterial agents on gamma-aminobutyric acid binding to receptor sites in rat brain membranes.
作者信息
Tsuji A, Sato H, Kume Y, Tamai I, Okezaki E, Nagata O, Kato H
机构信息
Faculty of Pharmaceutical Sciences, Kanazawa University, Japan.
出版信息
Antimicrob Agents Chemother. 1988 Feb;32(2):190-4. doi: 10.1128/AAC.32.2.190.
Abstract
The specific binding of 3H-labeled gamma-aminobutyric acid ([3H]GABA) to synaptic plasma membranes from rat brains was inhibited by various quinolonecarboxylic acid derivatives (quinolones), and these inhibitions were concentration dependent. The binding of [3H]muscimol to GABAA sites was also inhibited. These inhibitory potencies differed widely among the quinolones examined. The Dixon plots showed that a newly developed difluorinated quinolone, NY-198 [1-ethyl-6,8-difluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxo-3- quinolinecarboxylic acid hydrochloride], competitively inhibits the receptor bindings of [3H]GABA and [3H]muscimol. In conclusion, our findings suggest that the inhibition of GABA binding to receptors (including uptake sites) in the brain may be involved in the induction of epileptogenic neurotoxicities by quinolones.
摘要
3H标记的γ-氨基丁酸（[3H]GABA）与大鼠脑突触质膜的特异性结合受到多种喹诺酮羧酸衍生物（喹诺酮类）的抑制，且这些抑制作用呈浓度依赖性。[3H]蝇蕈醇与GABAA位点的结合也受到抑制。在所检测的喹诺酮类药物中，这些抑制效力差异很大。Dixon图表明，一种新开发的二氟喹诺酮NY-198 [1-乙基-6,8-二氟-1,4-二氢-7-(3-甲基-1-哌嗪基)-4-氧代-3-喹啉羧酸盐酸盐]竞争性抑制[3H]GABA和[3H]蝇蕈醇的受体结合。总之，我们的研究结果表明，喹诺酮类药物抑制大脑中GABA与受体（包括摄取位点）的结合可能与诱发性癫痫神经毒性有关。
相似文献
1
Inhibitory effects of quinolone antibacterial agents on gamma-aminobutyric acid binding to receptor sites in rat brain membranes.喹诺酮类抗菌剂对γ-氨基丁酸与大鼠脑膜受体位点结合的抑制作用。
Antimicrob Agents Chemother. 1988 Feb;32(2):190-4. doi: 10.1128/AAC.32.2.190.
2
Structure-epileptogenicity relationship of quinolones with special reference to their interaction with gamma-aminobutyric acid receptor sites.喹诺酮类药物的结构与致痫性的关系，特别提及它们与γ-氨基丁酸受体位点的相互作用。
Antimicrob Agents Chemother. 1989 Oct;33(10):1704-8. doi: 10.1128/AAC.33.10.1704.
3
Melatonin enhancement of [3H]-gamma-aminobutyric acid and [3H]muscimol binding in rat brain.褪黑素对大鼠脑中[3H]-γ-氨基丁酸和[3H]蝇蕈醇结合的增强作用。
Biochem Pharmacol. 1988 Apr 1;37(7):1271-4. doi: 10.1016/0006-2952(88)90781-2.
4
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.
5
Distribution and pharmacological properties of the GABAA/benzodiazepine/chloride ionophore receptor complex in the brain of the fish Anguilla anguilla.欧洲鳗鲡脑中γ-氨基丁酸A型/苯二氮䓬/氯离子载体受体复合物的分布及药理学特性
J Neurochem. 1989 Apr;52(4):1025-34. doi: 10.1111/j.1471-4159.1989.tb01843.x.
6
Indomethacin/ibuprofen-like anti-inflammatory agents selectively potentiate the gamma-aminobutyric acid-antagonistic effects of several norfloxacin-like quinolone antibacterial agents on [35S]t-butylbicyclophosphorothionate binding.消炎痛/布洛芬样抗炎药可选择性增强几种诺氟沙星样喹诺酮类抗菌药对[35S]叔丁基双环磷硫代酸盐结合的γ-氨基丁酸拮抗作用。
Mol Pharmacol. 1993 May;43(5):795-800.
7
Quinolones and fenbufen interact with GABAA receptor in dissociated hippocampal cells of rat.
J Neurophysiol. 1991 Aug;66(2):497-504. doi: 10.1152/jn.1991.66.2.497.
8
Biochemical evaluations of the effects of loreclezole and propofol on the GABAA receptor in rat brain.洛雷唑和丙泊酚对大鼠脑内GABAA受体作用的生化评估。
Biochem Pharmacol. 1996 Jun 14;51(11):1527-34. doi: 10.1016/0006-2952(96)00094-9.
9
10
Neurochemical studies on quinolone antibiotics: effects on glutamate, GABA and adenosine systems in mammalian CNS.
Pharmacol Toxicol. 1989 May;64(5):404-11. doi: 10.1111/j.1600-0773.1989.tb00676.x.
引用本文的文献
1
The First Case of Ceftazidime-Induced Antibiomania: A Case Report and Literature Review.首例头孢他啶诱发的抗生素躁狂症：病例报告及文献综述
Cureus. 2022 Dec 24;14(12):e32904. doi: 10.7759/cureus.32904. eCollection 2022 Dec.
2
Quinolone antibiotics and suicidal behavior: analysis of the World Health Organization's adverse drug reactions database and discussion of potential mechanisms.喹诺酮类抗生素与自杀行为：对世界卫生组织药品不良反应数据库的分析及潜在机制探讨
Psychopharmacology (Berl). 2016 Jul;233(13):2503-11. doi: 10.1007/s00213-016-4300-3. Epub 2016 Apr 26.
3
Reversible craniocervical dystonia associated with levofloxacin.与左氧氟沙星相关的可逆性颅颈肌张力障碍。
J Clin Mov Disord. 2015 May 4;2:10. doi: 10.1186/s40734-015-0021-8. eCollection 2015.
4
The Effect of Ciprofloxacin Injection on Genetically Absence Prone (Wag/Rij) Rat's Electroencephalogram Characteristics.环丙沙星注射液对遗传性失神发作易感（Wag/Rij）大鼠脑电图特征的影响。
Basic Clin Neurosci. 2013 Winter;4(1):31-5.
5
Evaluation of the possible epileptogenic activity of ciprofloxacin: the role of Nigella sativa on amino acids neurotransmitters.评价环丙沙星可能的致痫活性：黑种草子对氨基酸神经递质的作用。
Neurochem Res. 2013 Jan;38(1):174-85. doi: 10.1007/s11064-012-0905-z. Epub 2012 Oct 21.
6
Relative contributions of active mediated transport and passive diffusion of fluoroquinolones with various lipophilicities in a Calu-3 lung epithelial cell model.不同脂溶性氟喹诺酮类药物在 Calu-3 肺上皮细胞模型中主动介导转运和被动扩散的相对贡献。
Antimicrob Agents Chemother. 2010 Jan;54(1):543-5. doi: 10.1128/AAC.00733-09. Epub 2009 Oct 12.
7
The beneficial effect of N-acetylcysteine and ciprofloxacin therapy on the outcome of ischemic fulminant hepatic failure.N-乙酰半胱氨酸和环丙沙星治疗对缺血性暴发性肝衰竭预后的有益作用。
Dig Dis Sci. 2007 Dec;52(12):3507-10. doi: 10.1007/s10620-006-9594-2.
8
Norfloxacin-induced electroencephalogram alteration and seizures in rats are not triggered by enhanced levels of intracerebral glutamate.诺氟沙星引起的大鼠脑电图改变和癫痫发作并非由脑内谷氨酸水平升高所触发。
Antimicrob Agents Chemother. 2003 Nov;47(11):3660-2. doi: 10.1128/AAC.47.11.3660-3662.2003.
9
Clinically significant interactions with drugs used in the treatment of tuberculosis.与用于治疗结核病的药物存在具有临床意义的相互作用。
Drug Saf. 2002;25(2):111-33. doi: 10.2165/00002018-200225020-00005.
10
Convulsant and subconvulsant doses of norfloxacin in the presence and absence of biphenylacetic acid alter extracellular hippocampal glutamate but not gamma-aminobutyric acid levels in conscious rats.在清醒大鼠中，无论有无联苯乙酸存在，惊厥剂量和亚惊厥剂量的诺氟沙星均会改变细胞外海马谷氨酸水平，但不会改变γ-氨基丁酸水平。
Antimicrob Agents Chemother. 2002 Feb;46(2):471-7. doi: 10.1128/AAC.46.2.471-477.2002.
本文引用的文献
1
Solubilization of gamma-aminobutyric acid receptor from rat brain.从大鼠脑中溶解γ-氨基丁酸受体。
Life Sci. 1980 Apr 7;26(14):1131-7. doi: 10.1016/0024-3205(80)90652-9.
2
Inhibition of GABA and benzodiazepine receptor binding by penicillins.青霉素对γ-氨基丁酸（GABA）和苯二氮䓬受体结合的抑制作用。
Neurosci Lett. 1980 Jul;18(3):309-12. doi: 10.1016/0304-3940(80)90302-x.
3
Brain receptor binding and lipophilic character of benzodiazepines.苯二氮䓬类药物的脑受体结合及亲脂特性
Biochem Pharmacol. 1983 Feb 15;32(4):603-7. doi: 10.1016/0006-2952(83)90482-3.
4
3H-baclofen and 3H-GABA bind to bicuculline-insensitive GABA B sites in rat brain.3H-巴氯芬和3H-γ-氨基丁酸与大鼠脑中对荷包牡丹碱不敏感的γ-氨基丁酸B位点结合。
Nature. 1981 Mar 12;290(5802):149-52. doi: 10.1038/290149a0.
5
Effect of penicillin on transmitter release from rat cortical tissue.青霉素对大鼠皮质组织递质释放的影响。
Brain Res. 1980 Jun 16;192(1):296-300. doi: 10.1016/0006-8993(80)91033-1.
6
Gamma-aminobutyric acid binding to receptor sites in the rat central nervous system.γ-氨基丁酸与大鼠中枢神经系统中的受体位点结合。
Proc Natl Acad Sci U S A. 1974 Dec;71(12):4802-7. doi: 10.1073/pnas.71.12.4802.
7
In vitro and in vivo activity of NY-198, a new difluorinated quinolone.新型二氟喹诺酮NY-198的体外和体内活性
Antimicrob Agents Chemother. 1987 Jun;31(6):854-9. doi: 10.1128/AAC.31.6.854.
8
Comparative stereostructure-activity studies on GABAA and GABAB receptor sites and GABA uptake using rat brain membrane preparations.利用大鼠脑膜制备物对GABAA和GABAB受体位点以及GABA摄取进行的比较立体结构活性研究。
J Neurochem. 1986 Sep;47(3):898-903. doi: 10.1111/j.1471-4159.1986.tb00695.x.
9
Inhibitory effect of cephalosporins on gamma-aminobutyric acid receptor binding in rat synaptic membranes.头孢菌素对大鼠突触膜中γ-氨基丁酸受体结合的抑制作用。
Antimicrob Agents Chemother. 1985 Apr;27(4):650-1. doi: 10.1128/AAC.27.4.650.
10
Assay of proteins in the presence of interfering materials.在存在干扰物质的情况下对蛋白质进行分析。
Anal Biochem. 1976 Jan;70(1):241-50. doi: 10.1016/s0003-2697(76)80064-4.
Zotero 插件