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Expert Opin Ther Pat. 2010 Mar;20(3):291-305. doi: 10.1517/13543771003602004.

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

Author information

1
University of Arizona, Department of Pharmacology, 1501 N. Campbell Avenue, Tucson, Arizona 85724-5050, USA.

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.

PMID:
20180617
DOI:
10.1517/13543771003602004
[Indexed for MEDLINE]

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