FEMA 4774 is a positive allosteric modulator of taste receptors T1R2 and T1R3, two subunits of the human sweet taste receptor. FEMA 4774 is also used as a sucrose sweetness enhancer[1].
FEMA 4774 (0-50 μM) induces a dose-dependent decrease in the EC50 value of sucrose and significantly enhances the affinity of sucrose for its binding site with an α (effect of modulator on agonist affinity) value of 30 in the human sweet receptor cells[1].
FEMA 4774 (S9632) (oral gavage, 500-2000 mg/kg) does not cause a dose-dependent increase in polychromatic erythrocytes and induces micronuclei formation at dose levels up to 2000 mg/kg in Swiss albino (CD-1) mice[2].
The pharmacokinetic parameters of FEMA 4774 (S9632) in Male and Female Sprague-Dawley Rats
| Route | Day | Dose (mg/kg) | Sex | Cmax (ng/mL)±SD | Tmax (hr) | t1/2 (hr) | AUC0last(ng•hr/mL) | AUC0last/dose(ng•hr/mL/mg/kg) | %F |
| iv | 1 | 1.0 | M | 2036.7±281.9 | 0.03 | 0.19 | 330.6±58 | 330.6 | - |
| F | 2625.8±679.9 | 0.03 | 0.27 | 411.9±116.3 | 411.9 | - | |||
| Oral gavage | 1 | 10 | M | 12.9±3.2 | 0.25 | 1.21 | 17.9±2.3 | 1.79 | 0.54 |
| F | 34.0±3.9 | 0.25 | 1.17 | 49.2±7.8 | 4.92 | 1.19 | |||
| 30 | M | 90.0±23.9 | 0.33 | 0.88 | 90.8±11.0 | 3.03 | 0.92 | ||
| F | 62.4±25.9 | 0.42 | 1.06 | 95.0±20.4 | 3.17 | 0.77 | |||
| 100 | M | 147.2±86.3 | 0.33 | 0.71 | 176.2±73.8 | 1.76 | 0.53 | ||
| F | 268.5±90.7 | 0.25 | 0.99 | 341.1±81.0 | 3.41 | 0.83 | |||
| Oral gavage | 7 | 10 | M | 16.2±3.6 | 0.50 | 0.84 | 48.1±33.2 | 4.81 | - |
| F | 32.7±9.7 | 0.33 | 1.17 | 58.9±25.4 | 5.89 | - | |||
| 30 | M | 74.5±16.2 | 0.33 | 0.94 | 86.0±8.7 | 2.87 | - | ||
| F | 77.1±41.7 | 0.25 | 1.39 | 106.8±8.7 | 3.56 | - | |||
| 100 | M | 117.9±15.3 | 0.25 | 0.72 | 185.3±15.3 | 1.85 | - | ||
| F | 189.7±79.5 | 0.25 | 0.89 | 278.9±79.0 | 2.79 | - | |||