Discovery of Highly Selective 5-HT2A Agonists Using Structure-Guided Design

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Research shows enhanced selectivity for 5-HT2A over 5-HT2C receptors in psychedelics, suggesting advances in neuroplastic therapy.

Highly selective 5-HT2A agonists demonstrate improved target engagement, expanding psychedelic research.
Selectivity was confirmed using various assays including mouse head-twitch response tests and molecular docking.
Structure-based design achieved targeting of specific receptor residues, enhancing agonist effectiveness.
Findings contribute to understanding neurobiological mechanisms related to psychedelics and their therapeutic potentials.

Fenske et al. (2025) studied this question.

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