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novel 5-HT2A receptor agonists
- Development stage
- Preclinical
- Lead developer
- Atai Beckley
- Modality
- Small Molecules
- Administration
- Intracutaneous, Subcutaneous, Intravenous, Intraarterial, Intradermal, Transdermal, Oral, Sublingual, Buccal, Intranasal, Inhalation, Ocular, Intravascular, Cutaneous, Intramuscular, Intracranial, Epidural, Rectal, Intravesical, Vaginal, Intraperitoneal
01
Overview
Novel 5-HT2A receptor agonists (including non-hallucinogenic neuroplastogens) is a discovery-stage program being developed by ATAI Life Sciences (now AtaiBeckley) for the treatment of Opioid Use Disorder (OUD) and Treatment-Resistant Depression (TRD). These small molecule compounds are designed to act as agonists of the 5-HT2A and 5-HT2C receptors, specifically engineered to promote neuroplasticity without inducing the hallucinogenic effects typically associated with psychedelic substances. The program utilizes an AI-driven polypharmacology approach to optimize compounds for therapeutic efficacy while avoiding cardiac risks and hallucinogenic potential, as confirmed by preclinical drug discrimination studies. In September 2025, the program was awarded an $11.4 million grant from the National Institute on Drug Abuse (NIDA) to support its optimization and early-stage development for OUD.
- Other names
- non-hallucinogenic neuroplastogens5-HT2A/2C receptor agonists
02
Targets
HTR2C (5-hydroxytryptamine 2C receptor)HTR2A (Serotonin receptor 5-HT2A)HTR2B (5-Hydroxytryptamine Receptor 2B)
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