Cooper Medical School of Rowan University, Camden, NJ. United States.
CNS Neurol Disord Drug Targets. 2017;16(6):658-663. doi: 10.2174/1871527316666170207155149.
Chronic pain is treated most commonly with opioid analgesics, anti-inflammatory steroids and nonsteroidal anti-inflammatory drugs.
However, these compounds are not uniformly effective and their clinical use is constrained by unwanted side effects. GABAergic neurons are located in spinal nociceptive circuits suggesting that drugs with affinity at these receptors, including benzodiazepine-like drugs, may provide an alternative to opioids for the treatment of pain. However, systemically administered conventional benzodiazepines fail to produce antihyperalgesic effects, likely due to their concurrent sedative properties.
Recent evidence suggests that by targeting specific benzodiazepine-sensitive GABAA; receptor subtypes, the sedative properties of benzodiazepines can be circumvented and these compounds may be useful alternatives to opioids for the treatment of chronic pain.
The present review provides an overview of the GABAA; receptor subtypes involved in pain transmission as well as implications for the development of analgesic medications.
慢性疼痛最常使用阿片类镇痛药、抗炎类固醇和非甾体抗炎药进行治疗。
然而，这些化合物并非普遍有效，其临床应用受到不良反应的限制。γ-氨基丁酸能神经元位于脊髓伤害感受回路中，这表明这些受体具有亲和力的药物，包括苯二氮䓬类药物，可能为治疗疼痛提供一种替代阿片类药物的方法。然而，全身性给予常规苯二氮䓬类药物并不能产生抗痛觉过敏的作用，可能是由于它们同时具有镇静作用。
最近的证据表明，通过针对特定的苯二氮䓬敏感 GABAA；受体亚型，可以避免苯二氮䓬类药物的镇静作用，这些化合物可能是治疗慢性疼痛的阿片类药物的有用替代品。
本综述提供了参与疼痛传递的 GABAA；受体亚型的概述，以及对镇痛药物开发的影响。
