TABLE 3

[3H]Diprenorphine binding surfaces in hMOR-CHO cells

[3H]Diprenorphine binding surfaces were generated by displacing two concentrations of [3H]diprenorphine (0.08 and 0.47 nM) by nine concentrations of diprenorphine in the absence and presence of the indicated concentrations of either Salvinorin A or naloxone, generating 20 data points per experimental condition. The combined data of each condition (160 points for the Salvinorin A experiments, 120 points for the naloxone experiments) were fit to the one-site binding model using MLAB-PC for the best-fit estimates (± S.D.) of the Kd and Bmax values.


Test Drug

Bmax

Kd
nM fmol / mg protein ± S.D. nM ± S.D.
Salvinorin A (n = 4)
    0 288 ± 18 0.73 ± 0.04
    10,000 186 ± 18* 1.43 ± 0.11*
    40,000 190 ± 14* 1.56 ± 0.12*
Naloxone
    0 515 ± 25 0.97 ± 0.05
    10
445 ± 47
2.64 ± 0.25*
  • * P < 0.001 (F-test).