Identification and evaluation of a pinocembrin analog as a TRPV1 inhibitor with analgesic properties in murine pain models.

ABSTRACT:

Introduction

Pain is a complex phenomenon involving physiological and psychological responses to noxious stimuli. Long-term opioid or NSAID use leads to reduced efficacy and tolerance. Initially a thermosensitive receptor, TRPV1 is increasingly recognized as a target for analgesic intervention.

Methods

Our investigation is focused on the exploration of novel TRPV1 antagonists derived from natural sources through computational screening methodologies, aiming to assess their efficacy as analgesic agents.

Results

Among the compounds screened, a promising TRPV1 antagonist named pinocembrin-7-o-3-o-galloyl-4-6-hexahydroxydiphenoyl-beta-d-glucoside (PINO) has exhibited superior stability in its interaction with TRPV1 through virtual screening and molecular dynamics simulati

SUBMITTER: Chen H 

PROVIDER: S-EPMC12185462 | biostudies-literature | 2025

REPOSITORIES: biostudies-literature