Mar, 1995
LOCATION OF REGIONS OF THE OPIOID RECEPTOR INVOLVED IN SELECTIVE AGONIST BINDING
JOURNAL OF BIOLOGICAL CHEMISTRY
- ,
- ,
- Volume
- 270
- Number
- 12
- First page
- 6702
- Last page
- 6709
- Language
- English
- Publishing type
- DOI
- 10.1074/jbc.270.12.6702
- Publisher
- AMER SOC BIOCHEMISTRY MOLECULAR BIOLOGY INC
To elucidate which portions of the opioid receptor molecules are involved in the ligand selectivity, we have expressed chimeric receptors between the rat delta- and mu-opioid receptors from cDNAs and analyzed their ligand binding properties, We demonstrate that the major binding determinant for the delta-selective enkephalin related peptide, [D-Pen(2),D-Pen(5)]enkephalin, resides within the region comprising the transmembrane segments V-VII and the intervening loop regions, On the other hand, the region spanning from the intracellular loop I to the amino terminal half of the transmembrane segment III is shown to be involved in determining high-affinity binding of the mu-selective enkephalin-related peptides, [D-Ala(2),MePhe(4),Gly-ol(5)]enkephalin and [D-Ala(2), MePhe(4),Met-ol(5)]enkephalin, whereas the major determinant nant for binding of the mu-selective alkaloids, morphine and codeine, is demonstrated to exist in the region spanning the transmembrane segments V-VII, These results indicate that distinct regions of the opioid receptor determine the selectivity for the delta- and the mu-selective enkephalin-related peptides and that the binding determinant for the mu-selective alkaloids is distinct from that for the mu-selective enkephalin-related peptides.
- Link information
-
- DOI
- https://doi.org/10.1074/jbc.270.12.6702
- CiNii Articles
- http://ci.nii.ac.jp/naid/80008226118
- PubMed
- https://www.ncbi.nlm.nih.gov/pubmed/7896813
- Web of Science
- https://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=JSTA_CEL&SrcApp=J_Gate_JST&DestLinkType=FullRecord&KeyUT=WOS:A1995QQ85500044&DestApp=WOS_CPL
- ID information
-
- DOI : 10.1074/jbc.270.12.6702
- ISSN : 0021-9258
- CiNii Articles ID : 80008226118
- Pubmed ID : 7896813
- Web of Science ID : WOS:A1995QQ85500044