Table 2.
U-50488 series opioid receptor binding affinities (data from Loew et al. [35]).
| a Compound | MOR KD (nm) |
KOR KD (nm) |
Ratio MOR/KOR |
|---|---|---|---|
| U-50488H (2-(3,4-dichlorophenyl)-N-methyl- N-[(1S,2S)-2-(pyrrolidin-1-yl) cyclohexyl]acetamide) |
430 | 2.2 | 195 |
| U-51574 (2-(3,4-dichlorophenyl)-N-[(1R,2R)-2- (dimethylamino)cyclohexyl]-N- methylacetamide) |
220 | 71 | 3.1 |
| U-62066 (2-(3,4-Dichlorophenyl)-N-methyl-N- [(5R,7S,8S)-7-pyrrolidin-1-yl-1- oxaspiro[4.5]decan-8-yl] acetamide) |
210 | 2.5 | 85 |
| U-69593 (2-phenyl-N-methyl-N-[(5R,7S,8S) -7-pyrrolidin-1-yl-1-oxaspiro[4.5] decan-8-yl] acetamide) |
1700 | 7.2 | 236 |
a Loew et al. [35] did not specify stereochemistry of compounds tested; here we employ IUPAC naming of compounds.