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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Koutsoviti-Papadopoulou M, Kounenis G, Elezoglou V

Department of Pharmacology, Faculty of Veterinary Medicine, Aristotelian University, Thessaloniki, Greece.

Gen Pharmacol. 1995 Oct;26(6):1391-5. doi: 10.1016/0306-3623(95)00001-h.

In the present study the effect of flumequine, enoxacin and norfloxacin on the GABA-elicited contractions (EC50 1.10 x 10(-5) M) on the isolated guinea pig ileum was investigated, in a comparative manner. 2. All three fluoroquinolones dose-dependently antagonised the GABA-induced contractions in a non-competitive manner, but no statistical difference in the degree of the antagonism they produced was noted. Besides, they did not influence the ileal cholinergic contractions induced by exogenous acetylcholine. 3. These results suggest that the above fluoroquinolones tested dose-dependently inhibit the contractile effect of GABA on the guinea pig ileum and this inhibition seems to be associated with an antagonistic action of the fluoroquinolones at GABAA-receptors present in the guinea pig ileum.

在本研究中，以比较的方式研究了氟甲喹、依诺沙星和诺氟沙星对离体豚鼠回肠中γ-氨基丁酸（GABA）引发的收缩（半数有效浓度为1.10×10⁻⁵ M）的影响。2. 所有三种氟喹诺酮类药物均以非竞争性方式剂量依赖性地拮抗GABA诱导的收缩，但它们产生的拮抗程度没有统计学差异。此外，它们对外源性乙酰胆碱诱导的回肠胆碱能收缩没有影响。3. 这些结果表明，上述测试的氟喹诺酮类药物剂量依赖性地抑制GABA对豚鼠回肠的收缩作用，这种抑制似乎与氟喹诺酮类药物对豚鼠回肠中存在的GABAA受体的拮抗作用有关。

Koutsoviti-Papadopoulou M, Kounenis G, Elezoglou V

Department of Pharmacology, Faculty of Veterinary Medicine, Aristotelian University, Thessaloniki, Greece.

Gen Pharmacol. 1995 Oct;26(6):1391-5. doi: 10.1016/0306-3623(95)00001-h.

In the present study the effect of flumequine, enoxacin and norfloxacin on the GABA-elicited contractions (EC50 1.10 x 10(-5) M) on the isolated guinea pig ileum was investigated, in a comparative manner. 2. All three fluoroquinolones dose-dependently antagonised the GABA-induced contractions in a non-competitive manner, but no statistical difference in the degree of the antagonism they produced was noted. Besides, they did not influence the ileal cholinergic contractions induced by exogenous acetylcholine. 3. These results suggest that the above fluoroquinolones tested dose-dependently inhibit the contractile effect of GABA on the guinea pig ileum and this inhibition seems to be associated with an antagonistic action of the fluoroquinolones at GABAA-receptors present in the guinea pig ileum.

在本研究中，以比较的方式研究了氟甲喹、依诺沙星和诺氟沙星对离体豚鼠回肠中γ-氨基丁酸（GABA）引发的收缩（半数有效浓度为1.10×10⁻⁵ M）的影响。2. 所有三种氟喹诺酮类药物均以非竞争性方式剂量依赖性地拮抗GABA诱导的收缩，但它们产生的拮抗程度没有统计学差异。此外，它们对外源性乙酰胆碱诱导的回肠胆碱能收缩没有影响。3. 这些结果表明，上述测试的氟喹诺酮类药物剂量依赖性地抑制GABA对豚鼠回肠的收缩作用，这种抑制似乎与氟喹诺酮类药物对豚鼠回肠中存在的GABAA受体的拮抗作用有关。