Through our research efforts we have evaluated 1000+ compounds for their serotonin receptor binding profiles via 5-HTome, the majority of which can be categorized in two broad drug development programs: 1) Functionally selective 5-HT2C agonist with low 5-HT2A and 5-HT2B liability, and 2) Non-hallucinogenic 5-HT2A agonist with low 5-HT2B liability
Functionally Selective 5-HT2C Agonist
- Low nanomolar potency at the 5-HT2C receptor
- Low Activity/Inactivity at 5HT1A, 5-HT2A and 5-HT2B receptors
- 5-HT2C Gq-mediated signaling bias
- Minimal Beta-arrestin 1 and 2 recruitment
- Non-Hallucinogenic
- Therapeutic indications: schizophrenia; Alzheimer’s-induced psychosis; obesity
5-HT2C activation often leads to full, partial, or minimal beta-arrestin (5-HT2C-hβarr1 & 2) recruitment along with 5-HT2C-Gq activation, as shown in these typical binding profiles.
5-HT2A receptor agonist exhibiting multi-receptor selectivity
- Low nanomolar potency at the 5-HT2A and 5-HT2C receptors
- Inactive at 5-HT2B
- Non-Hallucinogenic
- Therapeutic indications: treatment-resistant depression (TRD); PTSD
