delta-Opioid receptor: the third extracellular loop determines naltrindole selectivity

X Li; E V Varga; D Stropova; T Zalewska; E Malatynska; R J Knapp; W R Roeske; H I Yamamura

doi:10.1016/0014-2999(96)00098-2

delta-Opioid receptor: the third extracellular loop determines naltrindole selectivity

Eur J Pharmacol. 1996 Apr 4;300(1-2):R1-2. doi: 10.1016/0014-2999(96)00098-2.

Authors

X Li¹, E V Varga, D Stropova, T Zalewska, E Malatynska, R J Knapp, W R Roeske, H I Yamamura

Affiliation

¹ Department of Pharmacology, College of Medicine, University of Arizona, Tucson 85724, USA.

PMID: 8741185
DOI: 10.1016/0014-2999(96)00098-2

Abstract

Human delta/mu-opioid receptor chimeras were constructed to determine the role of the second and third extracellular loops in alkaloid ligand selectivity. Exchanging the third extracellular loop of the delta-opioid receptor with that of the mu-opioid receptor dramatically decreased the affinity of naltrindole, but not that of morphine. The results suggest that different domains of the opioid receptor are involved in the binding of naltrindole and morphine.

Publication types

Research Support, Non-U.S. Gov't
Research Support, U.S. Gov't, P.H.S.

MeSH terms

Animals
Base Sequence
Binding Sites
Chimera
Chlorocebus aethiops
Humans
Molecular Sequence Data
Naltrexone / analogs & derivatives*
Naltrexone / metabolism
Narcotic Antagonists / metabolism*
Polymerase Chain Reaction
Receptors, Opioid, delta / chemistry
Receptors, Opioid, delta / metabolism*
Sequence Alignment

Substances

Narcotic Antagonists
Receptors, Opioid, delta
Naltrexone
naltrindole