Neuroactive steroids with potentiating effects on GABAA 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 5α- and 5β-reduced neuroactive steroids with either selective or combined modulatory action on GABAA 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.
- 5 α-Reduced neuroactive steroids
- 5 β-Reduced neuroactive steroids
- GABA channels
- Peripheral nociception
- T-type calcium channels
- Thermal and mechanical hyperalgesia