TABLE 2.
Anesthetic affinities for α1β3 GABAAR anesthetic-binding sites
IC50 values, the total anesthetic concentrations resulting in 50% inhibition of photolabeling of α1β3 GABAAR purified in 0.2 mm asolectin, 5 mm CHAPS, were determined as described under “Experimental Procedures” (mean ± range, two independent experiments); EC50 value for anesthesia, tadpole loss of righting reflex.
| Drug | R-[3H]Azietomidate IC50 | R-[3H]mTFD-MPAB IC50 | [3H]AziPm IC50 | EC50 anesthesia | Partition coefficient |
|---|---|---|---|---|---|
| μm | μm | μm | μm | ||
| R-Etomidate | 1.6 ± 0.3 2.5 ± 0.3a |
580 ± 110 | 0.5 ± 0.2 2.1 ± 0.5a |
2.3b | 300b |
| R-mTFD-MPAB | 69 ± 14 | 1.4 ± 0.4 | 0.7 ± 0.3 | 3.7c | 6,200c |
| Propofol | 13 ± 2 46 ± 3a |
44 ± 8 | 8 ± 2 25 ± 4a |
3d 4.7f (mg/kg) |
6,200e |
| AziPm | 10 ± 3 21 ± 4a |
8 ± 4 | 7 ± 2a | 3d | 8,500e |
| o-PD | 13 ± 2 | 54 ± 4 | NDf | 14.7f (mg/kg) | 4,900e |
a IC50 values for α1β3 GABAAR purified in 0.86 mm asolectin, 11.5 mm cholate are shown.
b From Ref. 26.
c From Ref. 25.
d From Ref. 21.
e XLOGP3 (46) was calculated with the ALOPS2.1 Program, VCCLAB, Virtual Computational Chemistry.
f Rat loss of righting reflex is shown in mg/kg (21); ND means not determined.