Novel Drug-Like Somatostatin Receptor 4 Agonists are Potential Analgesics for Neuropathic Pain.

ABSTRACT: Somatostatin released from the capsaicin-sensitive sensory nerves mediates analgesic and anti-inflammatory effects via the somatostatin sst₄ receptor without endocrine actions. Therefore, sst₄ is considered to be a novel target for drug development in pain including chronic neuropathy, which is an emerging unmet medical need. Here, we examined the in silico binding, the sst₄-linked G-protein activation on stable receptor expressing cells (1 nM to 10 μM), and the effects of our novel pyrrolo-pyrimidine molecules in mouse inflammatory and neuropathic pain models. All four of the tested compounds (C1-C4) bind to the same binding site of the sst₄ receptor with similar interaction energy to high-affinity reference sst₄ agonists, and they al

SUBMITTER: Kantas B 

PROVIDER: S-EPMC6940912 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature