Novel N-normetazocine Derivatives with Opioid Agonist/Sigma-1 Receptor Antagonist Profile as Potential Analgesics in Inflammatory Pain.

ABSTRACT: Although opioids and nonsteroidal anti-inflammatory drugs (NSAIDs) are the most common drugs used in persistent pain treatment; they have shown many side effects. The development of new analgesics endowed with mu opioid receptor/delta opioid receptor (MOR/DOR) activity represents a promising alternative to MOR-selective compounds. Moreover, new mechanisms, such as sigma-1 receptor (σ₁R) antagonism, could be an opioid adjuvant strategy. The in vitro σ₁R and σ₂R profiles of previous synthesized MOR/DOR agonists (-)-2R/S-LP2 (1), (-)-2R-LP2 (2), and (-)-2S-LP2 (3) were assayed. To investigate the pivotal role of N-normetazocine stereochemistry, we also synthesized the (+)-2R/S-LP2 (7)

SUBMITTER: Turnaturi R 

PROVIDER: S-EPMC9413390 | biostudies-literature | 2022 Aug

REPOSITORIES: biostudies-literature