新型GABAB拮抗剂CGP 35348可预防巴氯芬诱导的抗伤害感受和肌肉松弛作用。
CGP 35348, a new GABAB antagonist, prevents antinociception and muscle-relaxant effect induced by baclofen.
作者信息
Malcangio M, Ghelardini C, Giotti A, Malmberg-Aiello P, Bartolini A
机构信息
Department of Preclinical and Clinical Pharmacology, University of Florence, Firenze, Italy.
出版信息
Br J Pharmacol. 1991 Jun;103(2):1303-8. doi: 10.1111/j.1476-5381.1991.tb09784.x.
Abstract
- CGP 35348, a new GABAB antagonist, was examined on antinociception induced by (+/-)-baclofen by use of the hot plate and writhing tests in mice and the paw pressure test in rats. CGP 35348 was also studied in mice on (+/-)-baclofen-induced impairment of rota-rod performance. 2. CGP 35348, injected either i.p. (60-100 mg kg-1 in mouse) or intracerebroventricularly (i.c.v.) (0.5-2.5 micrograms per mouse; 25 micrograms per rat) prevented (+/-)-baclofen-induced antinociception. 3. CGP 35348 did not modify oxotremorine- and morphine-induced antinociception in mice and rats. 4. CGP 35348 (2.5 micrograms i.c.v. per mouse) also prevented (+/-)-baclofen-induced impairment of the rota-rod test. 5. Two other GABAB antagonists, phaclofen (50 micrograms i.c.v. per mouse) and 2-OH-saclofen (2.5 micrograms-10 micrograms i.c.v. per mouse) did not modify (+/-)-baclofen-induced antinociception. 7. These results suggest that, at present, CGP 35348 is the only compound able to antagonize (+/-)-baclofen-induced antinociception.
摘要
- 使用小鼠热板法、扭体试验以及大鼠足趾压痛试验，研究新型GABAB拮抗剂CGP 35348对(±)-巴氯芬诱导的抗伤害感受作用的影响。还在小鼠中研究了CGP 35348对(±)-巴氯芬诱导的转棒试验能力损伤的作用。2. 腹腔注射（小鼠剂量为60 - 100 mg/kg）或脑室内注射（小鼠每只0.5 - 2.5 μg；大鼠每只25 μg）CGP 35348均可阻断(±)-巴氯芬诱导的抗伤害感受作用。3. CGP 35348不改变小鼠和大鼠中奥索震颤素和吗啡诱导的抗伤害感受作用。4. CGP 35348（小鼠脑室内注射每只2.5 μg）也可阻断(±)-巴氯芬诱导的转棒试验损伤。5. 另外两种GABAB拮抗剂，即巴氯芬（小鼠脑室内注射每只50 μg）和2-羟基巴氯芬（小鼠脑室内注射每只2.5 μg - 10 μg）不改变(±)-巴氯芬诱导的抗伤害感受作用。7. 这些结果表明，目前CGP 35348是唯一能够拮抗(±)-巴氯芬诱导的抗伤害感受作用的化合物。
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