Arizona Health Sciences

Recently patented and promising ORL-1 ligands: where have we been and where are we going?

TitleRecently patented and promising ORL-1 ligands: where have we been and where are we going?
Publication TypeJournal Article
Year of Publication2010
AuthorsLargent-Milnes TM, Vanderah TW
JournalExpert Opin Ther Pat
Volume20
Issue3
Pagination291-305
Date Published2010 Mar
ISSN1744-7674
KeywordsAnalgesics, Animals, Drug Delivery Systems, Drug Design, Humans, Ligands, Narcotic Antagonists, Pain, Patents as Topic, Receptors, Opioid
Abstract

IMPORTANCE OF THE FIELD: The interactions of nociceptin/orphanin FQ (N/OFQ) and the opioid receptor-like receptor 1 (nociceptin opioid peptide--NOP) have been implicated in a variety of systems including cardiovascular, respiratory, immune, and the central and peripheral nervous systems.

AREAS COVERED IN THIS REVIEW: To elucidate the endogenous role of the N/OFQ-NOP system through the use of knockout and knockdown animal preparations, though most advances have been made using a host of synthetic agonists and antagonists. This review gives a brief history of the receptor-ligand discovery, the development of these agonists and antagonists within the last 10 years as published, and the therapeutic indications thereof focusing on pain.

WHAT THE READER WILL GAIN: The use of NOP ligands in pain has been controversial at best; however, there are indications that both agonists and antagonists have a place in the clinical setting for acute and chronic pain. NOP ligands have potential as novel therapeutics, interestingly, when incorporated into a rationally-designed multi-target agent.

TAKE HOME MESSAGE: The discovery of N/OFQ and NOP opened a new option for the treatment of pain with the potential for a decreased side effect profile. Numerous compounds have been designed to target this system, the most promising of which have mixed profiles.

DOI10.1517/13543771003602004
Alternate JournalExpert Opin Ther Pat
PubMed ID20180617
Faculty Member Reference: 
Tally Largent-Milnes, Ph.D.
Todd Vanderah, PhD