Liebman J M, Pastor G
Eur J Pharmacol. 1980 Feb 8;61(3):225-30. doi: 10.1016/0014-2999(80)90124-7.
The effects of intraventricularly administered baclofen and muscimol were investigated on tail-flick responding and on vocalization and motor responses to nociceptive pinch. Baclofen (1 microgram) and muscimol (0.1 microgram) strongly reduced responding to pinch, particularly vocalization, without altering tail-flick responding. When given systemically, however, baclofen markedly attenuated tail-flick as well as pinch responding. Muscimol produced only weak antinociception by systemic administration, suggesting that it may have poor access to brain. At antinociceptive doses, i. vent. muscimol produced less apparent muscle relaxation than did baclofen. These results suggest that baclofen's antinociceptive action may be mediated in part by a supraspinal, GABAergic substrate, in addition to a spinal component which may not directly involve GABA.
研究了脑室内注射巴氯芬和蝇蕈醇对甩尾反应以及对伤害性夹捏刺激的发声和运动反应的影响。巴氯芬(1微克)和蝇蕈醇(0.1微克)能强烈减少对夹捏刺激的反应,尤其是发声反应,而不改变甩尾反应。然而,当全身给药时,巴氯芬显著减弱甩尾反应以及对夹捏刺激的反应。蝇蕈醇全身给药仅产生微弱的抗伤害作用,提示其可能难以进入脑内。在抗伤害剂量下,脑室内注射蝇蕈醇产生的肌肉松弛比巴氯芬不明显。这些结果表明,巴氯芬的抗伤害作用除了可能不直接涉及GABA的脊髓成分外,可能部分由脊髓上的GABA能底物介导。