Phenethylaminylation: Preliminary In Vitro Evidence for the Covalent Transamidation of Psychedelic Phenethylamines to Glial Proteins using 3,5-Dimethoxy-4-(2-Propynyloxy)-Phenethylamine as a Model Compound DOI Creative Commons
Rajiv Rangan, Russell Petty, Suchismita Acharya

et al.

bioRxiv (Cold Spring Harbor Laboratory), Journal Year: 2025, Volume and Issue: unknown

Published: Feb. 17, 2025

Abstract Psychedelics are well known for their ability to produce profoundly altered states of consciousness. But, more importantly, the effects psychedelics can influence neurobehavioral changes that last after these acute subjective end. This phenomenon is currently being leveraged in development psychedelic-assisted psychotherapies treatment multiple neuropsychiatric disorders. The cellular and molecular mechanisms by which single doses able mediate long-term cognitive an active area research. We hypothesize contribute long term state covalently modifying proteins. post-translational modification possible through transglutaminase-mediated transamidation amine termini glutamine carboxamide residues. Here, we synthesize utilize a propargylated analogue mescaline – classic serotonergic psychedelic phenethylamine found cacti species identify putative protein targets modifications use click-chemistry primary human astrocyte cell culture model. Our preliminary findings indicate diverse array glial proteins may be substrates transglutaminase 2-mediated monoaminylation our model (“phenethylaminylation”). Based on points, speculatively highlight new directions study this noncanonical activity.

Language: Английский

Phenethylaminylation: Preliminary In Vitro Evidence for the Covalent Transamidation of Psychedelic Phenethylamines to Glial Proteins using 3,5-Dimethoxy-4-(2-Propynyloxy)-Phenethylamine as a Model Compound DOI Creative Commons
Rajiv Rangan, Russell Petty, Suchismita Acharya

et al.

bioRxiv (Cold Spring Harbor Laboratory), Journal Year: 2025, Volume and Issue: unknown

Published: Feb. 17, 2025

Abstract Psychedelics are well known for their ability to produce profoundly altered states of consciousness. But, more importantly, the effects psychedelics can influence neurobehavioral changes that last after these acute subjective end. This phenomenon is currently being leveraged in development psychedelic-assisted psychotherapies treatment multiple neuropsychiatric disorders. The cellular and molecular mechanisms by which single doses able mediate long-term cognitive an active area research. We hypothesize contribute long term state covalently modifying proteins. post-translational modification possible through transglutaminase-mediated transamidation amine termini glutamine carboxamide residues. Here, we synthesize utilize a propargylated analogue mescaline – classic serotonergic psychedelic phenethylamine found cacti species identify putative protein targets modifications use click-chemistry primary human astrocyte cell culture model. Our preliminary findings indicate diverse array glial proteins may be substrates transglutaminase 2-mediated monoaminylation our model (“phenethylaminylation”). Based on points, speculatively highlight new directions study this noncanonical activity.

Language: Английский

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