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Significance of GABAergic systems in the action of improgan, a non-opioid analgesic

机译：GABA能系统在非阿片类镇痛剂即兴的作用中的意义

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Improgan is the prototype drug from a new class of non-opioid analgesics chemically related to histamine and histamine antagonists, but the mechanism of action of these compounds has not been identified. Because several classes of analgesics act in the brain by reducing GABAergic inhibition of endogenous pain-relieving circuits; and because the activity of these substances is abolished by the GABA(A) agonist muscimol, the present study assessed the effects of muscimol on improgan antinociception in rats. Intracerebroventricular (icv) improgan (80 mug) and morphine (20 mug) both induced 80-100% of maximal analgesic responses on the tail flick test 10 to 30 min later. However, muscimol pretreatment (0.5 mug, icy) completely eliminated the antinociceptive activity of both compounds. Since improgan in vitro lacks activity at opioid and GABA, receptors, these findings: 1) confirm earlier literature showing that muscimol inhibits morphine analgesia, and 2) suggest that improgan activates a supraspinal, descending analgesic pathway, possibly via inhibition of GABAergic transmission. Since muscimol is the first compound discovered which inhibits improgan analgesia, muscimol will be a useful tool for the further characterization of this new class of pain-relieving substances. (C) 2001 Elsevier Science Inc. All rights reserved. [References: 24]
机译：Improgan是化学上与组胺和组胺拮抗剂化学相关的新型非阿片类镇痛药的原型药物，但尚未确定这些化合物的作用机理。因为通过减少GABA对内源性疼痛缓解回路的抑制作用，几种镇痛药在大脑中起作用;并且由于这些物质的活性已被GABA（A）激动剂麝香酚消灭，因此本研究评估了麝香酚对大鼠抗痛觉增强的作用。在10到30分钟后的甩尾试验中，脑室内（icv）即兴（80马克杯）和吗啡（20马克杯）均引起最大镇痛反应的80-100％。但是，麝香酚预处理（0.5马克杯，冰冷）完全消除了这两种化合物的镇痛作用。由于体外促生剂对阿片样物质和GABA受体缺乏活性，因此这些发现：1）证实早期文献显示麝香酚可抑制吗啡镇痛作用; 2）促成剂可能通过抑制GABA能传递来激活脊髓上，降压镇痛途径。由于麝香酚是第一个发现的抑制即席镇痛的化合物，因此麝香酚将成为进一步表征这类新型止痛物质的有用工具。 （C）2001 Elsevier Science Inc.保留所有权利。 [参考：24]

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