Linked Life Data

19646882

Source:http://linkedlifedata.com/resource/pubmed/id/19646882

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
17
pubmed:dateCreated
2009-8-21
pubmed:abstractText
A novel family of 1,3,5-trisubstituted 1,2,4-triazoles was discovered as potent and selective ligands for the delta opioid receptor by rational design. Compound 5b exhibited low-nanomolar in vitro binding affinity (IC(50)=5.8 nM), excellent selectivity for the delta opioid receptor over the alternative mu and kappa opioid receptors, full agonist efficacy in receptor down-regulation and MAP kinase activation assays, and low-efficacy partial agonist activity in stimulation of GTPgammaS binding. The apparent discrepancy observed in these functional assays may stem from different signaling pathways involved in each case, as found previously for other G-protein coupled receptors. More biological studies are underway to better understand the differential stimulation of signaling pathways by these novel compounds.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Sep
pubmed:issn
1464-3391
pubmed:author
pubmed:issnType
Electronic
pubmed:day
1
pubmed:volume
17
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
6442-50
pubmed:meshHeading
pubmed:year
2009
pubmed:articleTitle
Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.
pubmed:affiliation
Department of Pharmacology, University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School and the Informatics Institute of UMDNJ, Piscataway, NJ 08854, United States.
pubmed:publicationType
Journal Article