Linked Life Data

21036245

Source:http://linkedlifedata.com/resource/pubmed/id/21036245

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:dateCreated
2010-11-1
pubmed:abstractText
The ?-opioid receptor is the G protein coupled receptor (GPCR) responsible for the analgesic, rewarding and unwanted effects of morphine and similar drugs. Constitutive activity of GPCRs is a phenomenon that likely reflects receptors spontaneous adopting conformations that can activate G proteins, and is likely to be common to most if not all GPCRs. Basal constitutive activity has been observed in some systems with ?-opioid receptors, and constitutive activity is expressed by mutant ?-opioid receptors with amino acid substitutions in regions known to be important for signaling. However, ?-opioid receptors are unique in that a putative constitutively active state of the receptor, the ?*-state, has been suggested to be induced by prolonged agonist treatment. The ?*-state is thought to contribute to processes underlying adaptation to and withdrawal from opioid treatment, and may have a ligand sensitivity distinct from basal constitutive activity of the ?-opioid receptor or that exhibited by ?-opioid receptor mutants. In this chapter, we outline methods for measuring constitutively active ?-opioid receptors, including some that take advantage of the fairly direct coupling of the receptor to ion channels. We also briefly summarize the pharmacology of the different constitutively active ?-opioid receptor states, and highlight the areas where we need to know more. We hope that a better understanding of constitutive activity at the ?-opioid receptor may provide information useful in developing ligands that access subsets of receptor conformations, offering the potential to fine-tune opioid pharmacotherapy.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
1557-7988
pubmed:author
pubmed:copyrightInfo
Copyright © 2010 Elsevier Inc. All rights reserved.
pubmed:issnType
Electronic
pubmed:volume
484
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
445-69
pubmed:meshHeading
pubmed:year
2010
pubmed:articleTitle
Constitutively active ?-opioid receptors.
pubmed:affiliation
Australian School of Advanced Medicine, Macquarie University, New South Wales, Australia.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't, Research Support, N.I.H., Extramural