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

Tally M. Largent-Milnes, Todd W Vanderah

Research output: Contribution to journalArticle

33 Citations (Scopus)

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/OFQNOP 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 receptorligand 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.

Original languageEnglish (US)
Pages (from-to)291-305
Number of pages15
JournalExpert Opinion on Therapeutic Patents
Volume20
Issue number3
DOIs
StatePublished - Mar 2010

Fingerprint

Ligands
Pain
Opioid Peptides
Peripheral Nervous System
Acute Pain
Opioid Receptors
Cardiovascular System
Chronic Pain
Therapeutics
Central Nervous System
nociceptin receptor
nociceptin

Keywords

  • Multi-target approach
  • Nociceptin receptor
  • Nociceptin/opioid receptor-like receptor
  • Orphanin FQ
  • Pain

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmacology

Cite this

Recently patented and promising ORL-1 ligands : Where have we been and where are we going? / Largent-Milnes, Tally M.; Vanderah, Todd W.

In: Expert Opinion on Therapeutic Patents, Vol. 20, No. 3, 03.2010, p. 291-305.

Research output: Contribution to journalArticle

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