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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Analgesic, anticonvulsant and antioxidant activities of 3-[4-(3-trifluoromethyl-phenyl)-piperazin-1-yl]-dihydrofuran-2-one dihydrochloride in mice
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Analgesic, anticonvulsant and antioxidant activities of 3-[4-(3-trifluoromethyl-phenyl)-piperazin-1-yl]-dihydrofuran-2-one dihydrochloride in mice

机译：3- [4-（3-三氟甲基-苯基）-哌嗪-1-基]-二氢呋喃-2-酮二盐酸盐的镇痛，抗惊厥和抗氧化活性

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Recently we have shown that 3-[4-(3-trifluoromethyl-phenyl)-piperazin-1-yl] -dihydrofuran-2-one dihydrochloride (LPP1) is an antinociceptive and local anesthetic agent in rodents. Below an extended study of the pharmacological activity of LPP1 is described. In vitro LPP1 has no affinity for GABA A, opioidergic μ and serotonergic 5-HT 1A receptors. The total antioxidant capacity of LPP1 (1-10 mM) measured as ABTS radical cation-scavenging activity showed that LPP1 has dose-dependent antioxidant properties in vitro. Low plasma concentration of this compound detected by means of HPLC method 30 min after its intraperitoneal administration suggests a rapid conversion to metabolite(s) which may be responsible for its analgesic and anticonvulsant activities in vivo. In vivo the compound's influence on the electroconvulsive threshold and its activity in the maximal electroshock seizure test (MES) were evaluated. The results demonstrated that LPP1 had an anticonvulsant activity in the MES model (ED 50 = 112 mg/kg) and at a dose of 50 mg/kg was able to elevate the electroconvulsive threshold for 8 mA as compared to the vehicle-treated mice. The analgesic activity of LPP1 was investigated in the acetic acid-induced writhing test in two groups of mice: animals with sensory C-fibers ablated, and mice with C-fibers unimpaired. It proved the potent activity of this compound in both groups (approximately 85% as compared to the vehicle-treated mice). The adverse effects of LPP1 were evaluated as acute toxicity (LD 50 = 747.8 mg/kg) and motor coordination impairments in the rotarod and chimney tests. The results from these tests show that LPP1 at doses higher than 100 mg/kg is likely to impair the motor performance of experimental animals. Concluding, LPP1 is an analgesic and anticonvulsant compound which has antioxidant properties in vitro. Further studies are necessary to assess whether the antioxidant activity and the receptor profiling demonstrated in vitro can be confirmed for its metabolite(s) that are formed in vivo.
机译：最近，我们显示了3- [4-（3-三氟甲基-苯基）-哌嗪-1-基]-二氢呋喃-2-酮二盐酸盐（LPP1）在啮齿类动物中具有镇痛作用和局部麻醉作用。下面描述了LPP1药理活性的扩展研究。体外LPP1对GABA A，视蛋白μ和血清素能5-HT 1A受体没有亲和力。以ABTS自由基阳离子清除活性测量的LPP1的总抗氧化能力（1-10 mM）表明，LPP1在体外具有剂量依赖性的抗氧化性能。腹膜内给药后30分钟通过HPLC方法检测到的血浆血浆浓度低，表明该化合物迅速转化为代谢物，这可能是其体内止痛和抗惊厥活性的原因。在体内，评估了化合物对电惊厥阈的影响及其在最大电击惊厥试验（MES）中的活性。结果表明，LPP1在MES模型中具有抗惊厥活性（ED 50 = 112 mg / kg），与载体治疗的小鼠相比，在50 mg / kg的剂量下，LPP1可以提高8 mA的电惊厥阈值。在乙酸诱导的扭体试验中，在两组小鼠中研究了LPP1的镇痛活性：消融了感官C纤维的动物和未受损C纤维的小鼠。证明了该化合物在两组中均具有强效活性（与溶媒处理的小鼠相比约为85％）。 LPP1的不良反应被评估为急性毒性（LD 50 = 747.8 mg / kg）和在旋转脚架和烟囱测试中的运动协调障碍。这些测试的结果表明，高于100 mg / kg的LPP1剂量可能会损害实验动物的运动能力。最后，LPP1是一种止痛和抗惊厥化合物，在体外具有抗氧化特性。需要进一步的研究来评估是否可以证实其体内代谢物的抗氧化活性和受体分布在体外证明。

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