Positive Allosteric Modulators of Glycine Receptors and Their Potential Use in Pain Therapies.

ABSTRACT: Glycine receptors are ligand-gated ion channels that mediate synaptic inhibition throughout the mammalian spinal cord, brainstem, and higher brain regions. They have recently emerged as promising targets for novel pain therapies due to their ability to produce antinociception by inhibiting nociceptive signals within the dorsal horn of the spinal cord. This has greatly enhanced the interest in developing positive allosteric modulators of glycine receptors. Several pharmaceutical companies and research facilities have attempted to identify new therapeutic leads by conducting large-scale screens of compound libraries, screening new derivatives from natural sources, or synthesizing novel compounds that mimic endogenous compounds with antinociceptive activity. Advances in structural techniques

SUBMITTER: Gallagher CI 

PROVIDER: S-EPMC9553105 | biostudies-literature | 2022 Oct

REPOSITORIES: biostudies-literature