Targeting 5-HT7 Receptor with Biased Ligands to Alleviate Pain and Spinal Neuroinflammation - PubMed
4 hours ago
- #biased ligands
- #neuropathic pain
- #5-HT7 receptor
- The serotonin 5-HT7 receptor (5-HT7R) is a GPCR in the CNS, considered a promising target for treating CNS disorders like neuropathic pain and neuroinflammation.
- Biased ligands, such as Serodolin and MOA51, selectively activate specific 5-HT7R signaling pathways, offering potential therapeutic advantages in pain management.
- In inflammatory and neuropathic pain models, both Serodolin and MOA51 effectively reduced pain responses to a similar extent as pregabalin, without inducing tolerance after prolonged use.
- Treatment with 5-HT7R-biased ligands reduced spinal microglial activity and neuronal hyperactivity, indicating their ability to modulate neuroinflammatory processes in the spinal cord.
- These findings suggest 5-HT7R-biased ligands are promising analgesic candidates for alleviating both inflammatory and neuropathic pain by targeting neuroinflammation.