|Title||Recently patented and promising ORL-1 ligands: where have we been and where are we going?|
|Publication Type||Journal Article|
|Year of Publication||2010|
|Authors||Largent-Milnes TM, Vanderah TW|
|Journal||Expert Opin Ther Pat|
|Date Published||2010 Mar|
|Keywords||Analgesics, Animals, Drug Delivery Systems, Drug Design, Humans, Ligands, Narcotic Antagonists, Pain, Patents as Topic, Receptors, Opioid|
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.
|Alternate Journal||Expert Opin Ther Pat|
Recently patented and promising ORL-1 ligands: where have we been and where are we going?
Faculty Member Reference:
Tally Largent-Milnes, PhD
Todd Vanderah, Ph.D.