delta-Opioid receptor: the third extracellular loop determines naltrindole selectivity.
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.
Li
X
X
Department of Pharmacology, College of Medicine, University of Arizona, Tucson 85724, USA.
Varga
E V
EV
Stropova
D
D
Zalewska
T
T
Malatynska
E
E
Knapp
R J
RJ
Roeske
W R
WR
Yamamura
H I
HI
D000818:Animals; D001483:Base Sequence; D001665:Binding Sites; D002678:Chimera; D002522:Chlorocebus aethiops; D006801:Humans; D008969:Molecular Sequence Data; D009271:Naltrexone / Q000031:analogs & derivatives* / Q000378:metabolism; D009292:Narcotic Antagonists / Q000378:metabolism*; D016133:Polymerase Chain Reaction; D017465:Receptors, Opioid, delta / Q000737:chemistry / Q000378:metabolism*; D016415:Sequence Alignment
D009292:Narcotic Antagonists; D017465:Receptors, Opioid, delta; D009271:Naltrexone; C055382:naltrindole