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Biological studies of clavine alkaloids targeting CNS receptors

Summary

This paper reviews clavine alkaloids, a class of natural compounds from ergot fungi that show promise as psychiatric medications. Unlike well-known psychedelics like LSD, clavine alkaloids may provide therapeutic benefits for anxiety and depression without strong hallucinogenic effects. The authors highlight how these compounds interact with brain receptors in ways that could make them safer and more effective medications for treating mood and neurological disorders.

Background

Clavine alkaloids are ergot-derived compounds with potent physiological effects that have been understudied compared to well-established psychedelics like LSD and psilocybin. These compounds occur broadly in nature and possess greater conformational flexibility than lysergic acid derivatives, making them potentially superior receptor ligands.

Objective

This review presents current knowledge on biological properties of clavine alkaloids, compares their pharmacology to ergolines and related psychedelics, and demonstrates opportunities to develop novel structure-activity relationship profiles for medicinal chemistry studies and psychedelic therapeutics.

Results

Key clavine alkaloids including (+)-lysergol, (+)-isolysergol, and (+)-cycloclavine showed promising profiles with reduced hallucinogenic potential and good mood-regulating properties. These compounds demonstrated partial agonism at 5-HT receptors with reduced 5-HT2A activation compared to LSD while maintaining activity at therapeutically relevant receptors.

Conclusion

Clavine alkaloids represent a promising but understudied class of psychedelic compounds with potential for developing non-hallucinogenic therapeutic agents. Further SAR campaigns and in vivo studies are warranted to exploit their unique receptor binding profiles and expand the structurally limited portfolio of psychedelic therapeutics.
  • Published in:Frontiers in Psychiatry,
  • Study Type:Review,
  • Source: PMID: 38076698, DOI: 10.3389/fpsyt.2023.1286941
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