Molecular mechanisms of opioid receptor-dependent signaling and behavior.

Abstract:

:Opioid receptors have been targeted for the treatment of pain and related disorders for thousands of years and remain the most widely used analgesics in the clinic. Mu (μ), kappa (κ), and delta (δ) opioid receptors represent the originally classified receptor subtypes, with opioid receptor like-1 (ORL1) being the least characterized. All four receptors are G-protein coupled and activate inhibitory G proteins. These receptors form homo- and heterodimeric complexes and signal to kinase cascades and scaffold a variety of proteins.The authors discuss classic mechanisms and developments in understanding opioid tolerance and opioid receptor signaling and highlight advances in opioid molecular pharmacology, behavioral pharmacology, and human genetics. The authors put into context how opioid receptor signaling leads to the modulation of behavior with the potential for therapeutic intervention. Finally, the authors conclude there is a continued need for more translational work on opioid receptors in vivo.

journal_name

Anesthesiology

journal_title

Anesthesiology

authors

Al-Hasani R,Bruchas MR

doi

10.1097/ALN.0b013e318238bba6

subject

Has Abstract

pub_date

2011-12-01 00:00:00

pages

1363-81

issue

6

eissn

0003-3022

issn

1528-1175

journal_volume

115

pub_type

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