Table 1. Hypnotic activities of fluorine substituted phenyl acetate derivatives.
| Compd | R1 | R2 | Onset time (s) mean ± SD (n = 10) | Duration of LORR (s) mean ± SD (n = 10) | HD50 (mg/kg)a | LD50 (mg/kg)a | TI |
| 5a | CF3 | Et | 35.1±6.8 | 155.2±10.3 | 72.5 (67.9∼75.5) | 441.9 (437.7∼445.3) | 6.1 |
| 5b | CF3 | n-Pr | 32.4±5.6 | 162.6±15.7 | 58.7 (54.4∼63.4) | 346.4 (281.8∼387.5) | 5.9 |
| 5c | CF3 | CH2CF3 | N.A.b | N.A. | N.T.c | N.T. | N.T. |
| 5d | CH2CF3 | Et | 25.2±3.8 | 181.9±14.3 | 47.4 (42.3∼51.3) | 260.3 (199.2∼290.4) | 5.5 |
| 5e | CH2CF3 | n-Pr | 23.4±4.6 | 224.6±19.5 | 43.8 (38.9∼48.2) | 249.7 (191.8∼281.8) | 5.7 |
| 5f | CH2CF3 | CH2CF3 | N.A. | N.A. | N.T. | N.T. | N.T. |
| 5g | Me | CH2CF3 | 6.2±0.4 | 44.8±2.1 | 59.6 (40.0∼74.7) | 362.6 (319.2∼400.8) | 6.1 |
| 5h | Me | CH2CH2CF3 | 7.5±1.2 | 69.3±7.8 | 25.6 (25.4∼27.8) | N.T. | N.T. |
| 5i | Me | CH(CH3)CF3 | 7.2±0.5 | 80.1±9.3 | 21.1 (18.8∼23.1) | 111.9 (116.2∼119.8) | 5.5 |
| 5j | Et | CH2CF3 | 5.3±1.2 | 59.1±7.4 | 24.6 (22.7∼26.2) | 192.2 (149.5∼230.1) | 7.8 |
| 5k | Et | CH2CH2CF3 | 7.6±0.9 | 65.6±6.8 | 29.2 (28.8∼29.6) | N.T. | N.T. |
| 5l | Et | CH(CH3)CF3 | 7.3±1.1 | 121.2±11.5 | 20.7 (18.2∼22.3) | 103.4 (71.8∼116.8) | 5.1 |
| Propofol | 8.1±1.6 | 240.9±93.7 | 11.9 (11.7∼13.5) | 64.4 (56.9∼73.3) | 5.1 | ||
| Propanidid | 6.7±0.5 | 89.6±18.2 | 20.9 (18.6∼23.6) | 118.76 (112.0∼124.2) | 5.6 | ||
| AZD3043 | 5.6±1.2 | 63.8±8.5 | 17.6 (16.2∼19.6) | 98.4 (105.4∼112.5) | 6.0 |
a
95% confidence limits. bData not available. cData not tested. Data was expressed as means ± SD (n = 10).