Table 2. Comparison between Experimental and Calculated Efficacy Values for Compounds in Training Seta.
relative %Emax |
||
---|---|---|
name | exptl | calcd |
BW373U86 | 1.00 | 0.96 |
etorphine | 0.36 | 0.36 |
SIOM | 0.18 | 0.13 |
oxymorphindole | 0.12 | 0.04 |
diprenorphine | 0.08 | 0.01 |
buprenorphine | 0.00 | 0.13 |
naltrexone | 0.00 | 0.01 |
naltrindole | 0.00 | 0.04 |
(E)-BNTX | 0.00 | 0.07 |
Experimental data, except buprenorphine and naltrexone, is previously reported.29 Buprenorphine and naltrexone were experimentally designated %Emax = 0 values as both are classified as antagonists at the δ receptor.6,24 BW373U86 = (±)-4-((α-R*)-α-((2S*,5R*)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N,N-diethyl-benzamide, SIOM = 7-spiroindanyloxymorphone, (E)-BNTX = [(E)-benzylidenenaltrexone].