TABLE 1

Binding parameters of δ- or μ-OR in the presence or absence of the δ-i3L minigene

The specific binding of varying concentrations of [3H]diprenorphine (0.1–16 nM) [3H]DADLE (0.2–6 nM), and [3H]DAMGO (0.1–6 nM) was measured in membranes of HEK293 cells expressing the δ- or the μ-ORs after transient transfection with either empty vector (pcDNA3) or the minigene δ-i3L expression construct. Nonspecific binding was assessed in the presence of 10 μM naloxone.


Receptor Type

Expressed Plasmid

[3H]DADLE Binding

[3H]DAMGO Binding

[3H]Diprenorphine Binding
Kd
Bmax
Kd
Bmax
Kd
Bmax
nM pmol/mg nM pmol/mg nM pmol/mg
δ-OR pcDNA3 2.1 ± 0.9 0.4 ± 0.18 0.83 ± 0.3 2.02 ± 0.2
δ-OR δ-i3L 2.0 ± 0.4 0.25 ± 0.02 0.92 ± 0.2 2.15 ± 0.6
μ-OR pcDNA3 1.6 ± 0.3 0.9 ± 0.2 2.3 ± 0.3 5.48 ± 1.4
μ-OR
δ i3L


1.4 ± 0.2
0.6 ± 0.15
3.27 ± 0.8
5.82 ± 1.3