Binding and dissociation kinetic parameters of radiolabeled tracers ([125I]OXA and [3H]EMPA) and nonlabeled test compounds (lemborexant, almorexant, and suvorexant) on human OXRs
Data represent the mean ± S.E.M.
| hOX1R | hOX2R | |||||
|---|---|---|---|---|---|---|
| [125I]OXA | Lemborexant | [3H]EMPA | Lemborexant | Almorexant | Suvorexant | |
| kona (l · nmol−1 · min−1) | 0.0378 ± 0.0106 | 0.0262 ± 0.0028 | 0.0363 ± 0.0008 | 0.0496 ± 0.0010 | 0.0350 ± 0.0014 | 0.0052 ± 0.0002 |
| koffa (min−1) | 0.0423 ± 0.0016 | 0.2444 ± 0.0229 | 0.0578 ± 0.0014 | 0.0626 ± 0.0014 | 0.0022 ± 0.0003 | 0.0164 ± 0.0011 |
| Dissociation half-life (min) | 16.4 ± 1.0 | 2.8 ± 0.4 | 12.0 ± 0.5 | 11.1 ± 0.4 | 309 ± 55 | 42.2 ± 3.1 |
koff, dissociation rate constant.
↵a Harmonic mean.