TABLE 1

Summary of the effects of DAMGO, EGF, or DAMGO + EGF on DAMGO-stimulated GTPγS binding on wild-type or mutant Y166F MOR

Pharmacological data for DAMGO-stimulated GTPγS binding was collected on membranes taken from HEK cells stably transfected with either wild-type MOR (MOR) or the MOR mutant Y166F (Y166F). GTPγS binding was measured and analyzed as described under Materials and Methods. Results represent the means ± S.E.M. of four to eight independent experiments performed in triplicate. Data were analyzed by one-way ANOVA followed by Tukey's post hoc test. EC50 values were determined from nonlinear regression analysis (Prism version 4.0).

Treatment GroupEmaxEC50
% vehiclenM
MOR
    Vehicle96 ± 41.9 ± 0.21
    DAMGO61 ± 10*1.7 ± 0.39
    EGF56 ± 8*0.65 ± 0.37
    DAMGO + EGF23 ± 8***#N.A.
Y166F
    Vehicle100 ± 21.5 ± 0.23
    DAMGO71 ± 6*2.0 ± 0.22
    EGF95 ± 150.98 ± 0.26
    DAMGO + EGF60 ± 13*2.1 ± 0.38
  • N.A., not available.

  • * P < 0.05 versus vehicle.

  • *** P < 0.001 versus vehicle.

  • # P < 0.05 for DAMGO vs. DAMGO + EGF.