用于评估β-内酰胺类抗生素惊厥易感性的动物模型。
Animal model for evaluating the convulsive liability of beta-lactam antibiotics.
作者信息
Williams P D, Bennett D B, Comereski C R
机构信息
Department of Experimental Toxicology, Bristol-Myers Company, Syracuse, New York 13221-4755.
出版信息
Antimicrob Agents Chemother. 1988 May;32(5):758-60. doi: 10.1128/AAC.32.5.758.
Abstract
The beta-lactam antibiotics imipenem-cilastatin, BMY-26225, and cefazolin significantly lowered the convulsive threshold of pentylenetetrazole in mice. In addition, imipenem-cilastatin and cefazolin were found to inhibit 3H-labeled gamma-aminobutyric acid binding to synaptic membranes from rat brains. Our results suggest that the pentylenetetrazole convulsive model may be useful in evaluating the proconvulsive liabilities of new carbapenems and other beta-lactam antibiotics and that the mechanism of imipenem-cilastatin and cefazolin toxicity may involve interaction with gamma-aminobutyric acid receptors.
摘要
β-内酰胺类抗生素亚胺培南-西司他丁、BMY-26225和头孢唑林可显著降低小鼠戊四氮的惊厥阈值。此外，还发现亚胺培南-西司他丁和头孢唑林可抑制3H标记的γ-氨基丁酸与大鼠脑突触膜的结合。我们的结果表明，戊四氮惊厥模型可能有助于评估新型碳青霉烯类和其他β-内酰胺类抗生素的促惊厥风险，且亚胺培南-西司他丁和头孢唑林的毒性机制可能涉及与γ-氨基丁酸受体的相互作用。
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本文引用的文献
1
Protein measurement with the Folin phenol reagent.使用福林酚试剂进行蛋白质测定。
J Biol Chem. 1951 Nov;193(1):265-75.
2
Comparative assays of antiepileptic drugs in mice and rats.小鼠和大鼠中抗癫痫药物的比较试验。
J Pharmacol Exp Ther. 1952 Nov;106(3):319-30.
3
Seizures associated with high cerebrospinal fluid concentrations of cefazolin.与脑脊液中头孢唑林高浓度相关的癫痫发作。
Am J Hosp Pharm. 1980 Feb;37(2):271-3.
4
Epileptogenic activity of cephalosporins in rats and their structure-activity relationship.头孢菌素在大鼠中的致痫活性及其构效关系。
Epilepsia. 1983 Aug;24(4):431-9. doi: 10.1111/j.1528-1157.1983.tb04913.x.
5
A new model of experimental epilepsy: the cefazolin-induced epilepsy.一种新的实验性癫痫模型：头孢唑林诱导的癫痫。
Prog Clin Biol Res. 1983;124:129-44.
6
Convulsive action of penicillin.青霉素的惊厥作用。
Brain Res. 1972 Aug 11;43(1):242-5. doi: 10.1016/0006-8993(72)90288-0.
7
Neurotoxicity of intravenously administered penicillin G.静脉注射青霉素G的神经毒性
Arch Neurol. 1971 Sep;25(3):232-9. doi: 10.1001/archneur.1971.00490030058006.
8
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.
9
Comparative convulsant activity of various penicillins after intracerebral injection in mice.
J Pharm Pharmacol. 1973 Feb;25(2):104-8. doi: 10.1111/j.2042-7158.1973.tb10602.x.
10
Primaxin in the treatment of acute bacterial pneumonia in adults.普米克令舒用于治疗成人急性细菌性肺炎。
J Antimicrob Chemother. 1985 Feb;15(2):233-8. doi: 10.1093/jac/15.2.233.
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