Table 1. In Vitro Affinity and Functional Activity of FPT at 5-HT1ARs, 5-HT2CRs, and 5-HT7Rsa.
receptor | Ki | EC50 | Emax |
---|---|---|---|
5-HT1A | 4.0 ± 0.1b | 37.4 ± 6.8 | 84 ± 1.4 |
5-HT2C | 243 ± 23 | 307 ± 76 | 68.4 ± 3.6 |
5-HT7 | 5.3 ± 2b | 4.2 ± 2.1 | 21.8 ± 3.9 |
Affinities are reported as the equilibrium dissociation constants (Ki) in nM, determined from radioligand competition binding assays. Functional potency is expressed as the EC50 (nM) and efficacy as Emax (% normalized to the full agonists 5-CT for 5-HT1ARs, 5-HT7Rs or 5-HT for 5-HT2CRs). Data were derived from at least three independent experiments.
Data are also reported in Perry et al. 2020.96