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Vol. 283, Issue 2, 501-510, 1997
Departments of
Pharmacology (M.J.C., P.J.E., J.H.W., A.E.R., F.M.),
Biological Chemistry (F.M.),
Psychology (J.H.W.), and
Mental Health
Research Institute (A.M., H.A.) University of Michigan, Ann Arbor,
Michigan, and
Department of Medicinal Chemistry (P.S.P.),
College of
Pharmacy, and Department of Pharmacology (P.S.P.), Medical School,
University of Minnesota, Minneapolis, Minnesota
A C6 glioma cell line stably transfected with the rat
delta opioid receptor (C6
) was used to characterize
receptor binding and G protein activation by both peptide and
nonpeptide delta opioid ligands. The ligand binding
affinities for [3H]naltrindole and
[3H]pCl-[D-Pen2,D-Pen5]enkephalin
(DPDPE) were similar to those observed in monkey brain membranes. The
nonpeptide agonists, BW373U86 and SNC80, as well as peptide agonist
[D-Ser2,L-Leu5]enkephalyl-Thr
maximally stimulated [35S]GTP
S binding by 640, 654 and
576%, respectively, over basal. The peptide agonists, DPDPE and
deltorphin II, both stimulated [35S]GTPS binding by
375%. Etorphine, diprenorphine, oxymorphindole and
7-spiroindanyloxymorphone were also partial agonists in this assay,
although they were less efficacious than deltorphin II. Stimulation of
[35S]GTPS binding by agonists was blocked completely
by pertussis toxin pretreatment. Both delta-1 and
delta-2 selective antagonists 7-benzylidenenaltrexone
and a benzofuran analog of naltrindole displayed high affinity for the
cloned receptor (0.04 and 0.08 nM) and antagonized the stimulation of
[35S]GTPS binding by BW373U86 and DPDPE with similar
potencies. Other evidence suggesting the lack of receptor subtypes
includes the finding that stimulation of [35S]GTPS
binding by receptor subtype selective ligands DPDPE and deltorphin II
was not additive. BW373U86, SNC80 and DPDPE maximally inhibited
forskolin-stimulated adenylyl cyclase. These cells highly express a
homogeneous population of delta opioid receptor that couple to inhibitory Go/Gi proteins. Ligand
affinity for the delta opioid receptor correlates with
ligand EC50 values for stimulation of
[35S]GTPS binding.
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