Compound | Ki | IC50 | GFT EC50 | GFT EC90 | % Receptor Occupancy at EC90 |
---|---|---|---|---|---|
nM | mg/kg | ||||
L-742,694 | 0.018 | 0.28 | 0.12 | 0.3 | 45 |
L-760,735-F | 0.197 | 0.15 | 0.25 | 1 | 80 |
MK-869 | 0.070 | 0.43 | 0.06 | 1 | 65 |
GR205171 | 0.016 | 1.25 | 0.29 | 1 | 45 |
L-733,060 | 0.083 | 1.14 | 2.06 | 10 | 90 |
CP-122,721 | 0.035 | 7.61 | 2.09 | 10 | 60 |
CP-99994 | 0.145 | 36.8 | 10.6 | 30 | 40 |
L-733,061 | 165 | >30 | >30 |
The IC50 column refers to the dose of antagonist that inhibited125I-SP binding 50% ex vivo. The EC50 for gerbil foot tapping represents the dose at which 50% inhibition of the behavioral response occurs. The GFT EC90 is the dose of antagonist at which the response is almost maximally inhibited. Receptor occupancy at the GFT EC90 was estimated by extrapolating from this dose to the intercept on the appropriate ex vivo binding inhibition curve then calculating the percentage of inhibition of ex vivo 125I-SP binding as a measure of receptor occupancy (see text for details).