Case Study

Comparison of hallucinogenic versus non-hallucinogenic psychedelics on 5HT2A receptors

Unlock new potential in 5HT2A receptor drug discovery with SB Drug Discovery’s advanced cell-based assay suite, meticulously designed to profile and differentiate serotonergic ligands. Leveraging assays that assess calcium mobilization, β-arrestin recruitment, and pERK signaling, alongside extensive subtype selectivity and receptor internalization assays, this platform provides a robust foundation for examining hallucinogenic and non-hallucinogenic compound interactions.

Introduction

Serotonergic psychedelics, known for their impact on mood, perception, and cognitive processes, primarily target the serotonin (5HT) 2A receptor subtype. While these psychedelics have garnered attention for their therapeutic potential, their exploration has been hindered by their spectre of adverse effects. Issues such as disorientation, anxiety, hallucinations, seizures, and, in extreme cases, fatalities have tempered widespread investigation of their clinical application.

The 5HT2A receptor functions via various ntracellular signalling pathways, including the canonical Gq-coupled pathway and β-arrestin recruitment, each contributing to distinct physiological effects. It has been suggested that ligands showing functional bias towards specific signalling pathways may allow separation of the desired therapeutic effect from unwanted side effects, offering the potential to develop effective ligands that can be used to target specific neuropathological conditions.

Comparison of hallucinogenic versus non-hallucinogenic psychedelics on 5HT2A receptors

Figure 1: 5HT2A receptor signalling pathways.

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