Identification of the amino acid residues involved in selective agonist binding in the first extracellular loop of the δ‐ and μ‐opioid receptors
- 9 October 1995
- journal article
- research article
- Published by Wiley in FEBS Letters
- Vol. 373 (2), 177-181
- https://doi.org/10.1016/0014-5793(95)01034-c
Abstract
Effects of amino acid substitutions in the first extracellular loop region of the β- and μ-opioid receptors were examined. Substitution of lysine-108 of the δ-receptor (δK108) with asparagine improved affinity to [d-Ala2,MePhe4,Gly-ol5]enk ephalin (DAGO), a μ-selective peptide agonist, to be comparable with that of the μ-receptor. On the other hand, replacement of mN127 with lysine decreased the affinity to DAGO by ∼ 15-fold. These results suggest that dK108 and mN127, which correspond to each other in the aligned amino acid sequences, mainly determine the difference in DAGO binding affinity between the δ- and μ-receptorsKeywords
This publication has 18 references indexed in Scilit:
- DAMGO, a μ‐opioid receptor selective ligand, distinguishes between μ‐and κ‐opioid receptors at a different region from that for the distinction between μ‐ and δ‐opioid receptorsFEBS Letters, 1995
- A Chimeric Study of the Molecular Basis of Affinity and Selectivity of the κ and the δ Opioid Receptors.Journal of Biological Chemistry, 1995
- Location of Regions of the Opioid Receptor Involved in Selective Agonist BindingPublished by Elsevier ,1995
- DAMGO, a μ‐opioid receptor selective agonist, distinguishes between μ‐ and δ‐opioid receptors around their first extracellular loopsFEBS Letters, 1995
- cDNA cloning and pharmacological characterization of an opioid receptor with high affinities for κ‐subtype‐selective ligandsFEBS Letters, 1993
- Primary structures and expression from cDNAs of rat opioid receptor δ‐and μ‐subtypesFEBS Letters, 1993
- Molecular Characterization of Opioid ReceptorsAnnual Review of Pharmacology and Toxicology, 1990
- The Molecular Basis of Opioid Receptor FunctionEndocrine Reviews, 1988
- Expression of functional acetylcholine receptor from cloned cDNAsNature, 1984
- Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reactionBiochemical Pharmacology, 1973