Abstract:
BACKGROUND AND RATIONALE:Pain is a complex sensory experience, involving cognitive factors, environment (setting, society, and culture), experience, and gender and is modulated significantly by the central nervous system (CNS). The mechanisms by which opioid analgesics work are understood, but this class of drugs is not ideal as either an analgesic or anti-hyperalgesic. Accordingly, considerable effort continues to be directed at improved understanding of nociceptor function and development of selective analgesics that do not have the unwanted effects associated with opioid analgesics. OBJECTIVE:The purpose of this paper is to provide a review of the role of KOP receptors in the modulation of pain and highlight several chemotypes currently being explored as peripherally restricted KOP ligands. RESULTS:A growing body of literature has shown that KOP receptors are implicated in a variety of behavioral pain models. Several different classes of peripherally restricted peptidic and nonpeptidic KOP agonists have been identified and show utility in treating painful conditions. CONCLUSION:The pharmacological profile of KOP agonists in visceral pain models suggest that peripherally restricted KOP agonists are potentially useful for a variety of peripheral pain states. Further, clinical investigation of peripherally restricted KOP agonists will help to clarify the painful conditions where KOP agonists will be most effective.
journal_name
Psychopharmacology (Berl)journal_title
Psychopharmacologyauthors
Kivell B,Prisinzano TEdoi
10.1007/s00213-010-1819-6subject
Has Abstractpub_date
2010-06-01 00:00:00pages
109-19issue
2eissn
0033-3158issn
1432-2072journal_volume
210pub_type
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