TABLE 1

Competition of [3H]14-methoxymetopon and [3H]DAMGO binding by various opioid agonists and antagonists Competition binding was performed against 1 nM [3H]14-methoxymetopon and 1 nM [3H]DAMGO with the stated opioid. IC50 values were determined and converted to Ki values as described under Materials and Methods. Results are mean ± S.E.M. of three independent experiments. Two-way analysis of variance followed by Bonferroni's post-tests shows that agonist do not differ in their ability to compete [3H]14-methoxymetopon versus [3H]DAMGO.




[3H]14-Methoxymetopon Ki

[3H]DAMGO Ki
nM
14-Methoxymetopon 0.30 ± 0.03 0.14 ± 0.02
Morphine 3.9 ± 0.7 1.25 ± 0.29
DAMGO 1.32 ± 0.10 0.60 ± 0.09
M6G 6.9 ± 1.6 5.46 ± 1.42
[d-Pen2,d-Pen5]-enkephalin >400 >250
U50,488H >400 >350
Naloxone 1.65 ± 0.24 0.35 ± 0.15
d-Phe-Cys-Tyr-d-Trp-Arg-Thr-Pen-Thr-NH2 (CTAP) 1.84 ± 0.28 7.24 ± 3.24
Naloxonazine 2.53 ± 0.28 1.84 ± 6.48
3-Methoxynaltrexone
>200
>600