Table 3. Variation of Substituents at Major Metabolic Positions, Region B.
% inhibition
@ 1 μM or Ki (nM) |
|||||
---|---|---|---|---|---|
compd | R1 | R2 | config | hNOPr | hMOPr |
3aa | F | Me | trans | 0.9 | 0.7 |
3ba | F | Me | cis | 97.4 | 46 |
4aa | F | H | trans | 11 | 2 |
47aa | Me | Me | trans | 4.5 | 2.7 |
48aa | OH | Me | trans | 1 | 0.4 |
49ab | OMe | Me | trans | 9.4 | 1.1 |
Hemicitrate.
Hydrochloride.