Department of Anesthesiology, University of Virginia Health System, PO Box 800710, Charlottesville, VA, USA.
Psychoneuroendocrinology. 2009 Dec;34 Suppl 1:S178-85. doi: 10.1016/j.psyneuen.2009.06.001.
Neuroactive steroids with potentiating effects on GABA(A) channels and inhibitory effects on T-type Ca2+ channels which are located in peripheral sensory neurons are potent modulators of pain perception. The focus of this review is on peripheral anti-nociceptive properties of 5alpha- and 5beta-reduced neuroactive steroids with either selective or combined modulatory action on GABA(A) and T-type Ca2+ channel-mediated neurotransmission. We report that these neuroactive steroids are very effective in alleviating peripheral nociception in both acute and chronic pain conditions in animal models of pain. We believe that promising animal data warrant the exploration of their usefulness in clinical settings especially considering the fact that chronic pain sufferers are often young and otherwise healthy people.
具有增强 GABA(A) 通道作用和抑制 T 型钙通道作用的神经活性甾体位于周围感觉神经元中,是疼痛感知的有效调节剂。本综述的重点是具有 GABA(A) 和 T 型钙通道介导的神经传递的选择性或组合调节作用的 5α-和 5β-还原神经活性甾体的外周抗伤害感受特性。我们报告说,这些神经活性甾体在疼痛动物模型的急性和慢性疼痛条件下非常有效地缓解外周伤害感受。我们相信,有希望的动物数据证明了它们在临床环境中的有用性值得探索,特别是考虑到慢性疼痛患者通常是年轻且健康的人这一事实。