Linked Life Data

7768887

Source:http://linkedlifedata.com/resource/pubmed/id/7768887

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
22
pubmed:dateCreated
1995-7-5
pubmed:abstractText
To investigate the interaction between the mu opioid receptor and its ligands, we compared the binding of mu-selective ligands to two mu/kappa chimeric opioid receptors and to mu and kappa receptors. The two chimeras were constructed from cloned rat mu and kappa receptors in which a segment from the middle of the third intracellular loop to the C terminus was exchanged. When this portion of the kappa receptor was replaced by that of the mu receptor, affinities of mu selective agonists, DAMGO (Tyr-D-Ala-Gly-NMePhe-Gly-ol), PL017 (Tyr-Pro-NMePhe-D-Pro-NH2), sufentanil, and morphine, were greatly increased as compared to those for the kappa receptor. Conversely, when this region of the mu receptor was substituted by that of the kappa receptor, affinities for these agonists were substantially decreased as compared with those of the mu receptor. Unlike selective agonists, the mu-selective antagonist, CTAP (D-Phe-Cys-Tyr-D-Trp-Arg-Thr-penicillamine-Thr-NH2), displayed a low affinity for both chimeric receptors, similar to that of the kappa receptor. Thus, the region from the middle of the third intracellular loop to the C terminus of the mu receptor is important for the binding of selective agonists. Conversely, the determinants for selective binding of the antagonist CTAP reside in a more extended region of the receptor.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jun
pubmed:issn
0021-9258
pubmed:author
pubmed:issnType
Print
pubmed:day
2
pubmed:volume
270
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
12977-9
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
1995
pubmed:articleTitle
The third extracellular loop of the mu opioid receptor is important for agonist selectivity.
pubmed:affiliation
Department of Pharmacology, Temple University School of Medicine, Philadelphia, Pennsylvania 19140, USA.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S., Research Support, Non-U.S. Gov't