Abstract

Rita Mourya*, Ansari Arshi Shakeel Ahmed

ABSTRACT

Opiorphin, an endogenous pentapeptide discovered in human saliva, has emerged as a promising analgesic and therapeutic agent. Opiorphin functions as an inhibitor of enkephalin-degrading enzymes, thereby enhancing the body's natural pain-relieving mechanisms. This comprehensive review examines its biochemical properties, pharmacological potential, and therapeutic applications in both preclinical and clinical settings. Opiorphin's unique interaction with opioid receptors—occurring indirectly through enkephalin protection rather than direct receptor activation—provides an innovative approach to pain management without inducing addiction or tolerance. The peptide demonstrates remarkable efficacy across various pain models, including acute, inflammatory, neuropathic, and visceral pain. Beyond analgesia, opiorphin shows promise in treating anxiety, depression, and chronic stress disorders, further expanding its clinical applications. Pharmacokinetic and pharmacodynamic studies have elucidated its metabolism and administration routes, while safety profiles suggest significantly fewer side effects than conventional opioid drugs. However, important research gaps remain, particularly regarding human clinical trials, pharmaceutical formulations, and long-term safety assessments. This review discusses the current landscape, potential challenges, and future directions for opiorphin research, emphasizing its potential role in reshaping modern pain management strategies while addressing the ongoing opioid crisis.