Title:Innovative Opioid Peptides and Biased Agonism: Novel Avenues for More Effective and Safer Analgesics to Treat Chronic Pain
Volume: 25
Issue: 32
Author(s): Andrea Bedini*Santi Spampinato
Affiliation:
- Department of Pharmacy and Biotechnology (FaBiT), University of Bologna, Bologna,Italy
Keywords:
Mu opioid receptor, delta opioid receptor, kappa opioid receptor, endomorphin, dermorphin, biased
agonism, innovative analgesics.
Abstract: Background: Chronic pain states are clinically relevant and yet unsolved conditions
impacting on quality of life and representing an important social and economic burden;
these diseases are poorly treated with the currently available drugs, being urgent the need of
innovative analgesics.
In this frame, novel analogues of endomorphin-1 and dermorphin emerge as promising starting
points to develop innovative, more effective analgesics to treat neuropathic pain.
Methods: An extensive and structured search of bibliographic databases for peer-reviewed
research literature was undertaken using focused review questions; all the retrieved papers
were published on prestigious international journals by the experts of the field and were
carefully analyzed to collect all the information and data necessary to the conceptual framework
of this review.
Results: One hundred papers were included in this review; forty-one defined the up-to-date
findings on neuropathic pain etiopathogenesis and its currently available treatment options.
Thirty-five papers described all the advantages and drawbacks of using endomorphin-1 (23)
or dermorphin (12) in the frame of neuropathic pain and outlined the most relevant advances
in developing endomorphin-1 and dermorphin analogs useful as potential, innovative analgesics.
Twenty-four papers provided the latest insights into exploiting biased agonism at opioid receptor
as an innovative strategy to develop more effective and safer analgesics.
Conclusion: This review reports that innovative opioid peptides will be of great help in better
understanding the multifaceted scenario of neuropathic pain treatment, providing very
interesting opportunities for the identification of novel and more effective opioid analgesics
to be employed as medications.
