Table 2. Kinetic Binding Parameters of Radioligands and Unlabeled FPT at 5-HT1ARs, 5-HT2CRs, and 5-HT7Rsa.
receptor | compound | residence time | koff | kon | Kd |
---|---|---|---|---|---|
5-HT1A | [3H]5-CT | 3 | 0.32 ± 0.06 | 1.3 × 108 ± 3.3 × 107 | 2.5 |
FPT | 2 | 0.50 ± 0.04 | 2.8 × 107 ± 8.6 × 106 | 18 | |
5-HT2C | [3H]mesulergine | 143 | 0.007 ± 0.001 | 4.1 × 106 ± 2.2 × 105 | 1.7 |
FPT | 5 | 0.186 ± 0.018 | 2.5 × 105 ± 1.9 × 104 | 732 | |
5-HT7 | [3H]5-CT | 143 | 0.007 ± 0.002 | 2.3 × 107 ± 2.9 × 106 | 0.3 |
FPT | 4 | 0.26 ± 0.12 | 4.3 × 107 ± 1.8 × 107 | 6.2 |
koff (min–1) and kon (M–1·min–1) were derived from 3–4 independent experiments. Residence time was calculated as 1/koff and was rounded to the nearest minute, while the kinetically determined Kd was calculated using mean kinetic parameters and the equation Kd = koff/kon, presented in nM.