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Hailey A. Bock

5 papers in the library · 239 citations · publishing 2022-2024

Papers

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Bioisosteric analogs of MDMA: Improving the pharmacological profile?

Journal of Neurochemistry September 1, 2024 Ana Sofia Alberto-Silva, Selina Hemmer, Hailey A. Bock et al. 10 citations

3,4-Methylenedioxymethamphetamine (MDMA, 'ecstasy') is re-emerging in clinical settings as a candidate for the treatment of specific neuropsychiatric disorders (e.g. post-traumatic stress disorder) in combination with psychotherapy. MDMA is a psychoactive drug, typically regarded as an empathogen or entactogen, which leads to transporter-mediated monoamine release. Despite its therapeutic...

Bioisosteric analogs of MDMA with improved pharmacological profile.

bioRxiv : the preprint server for biology April 11, 2024 Ana Sofia Alberto-Silva, Selina Hemmer, Hailey A. Bock et al. preprint

3,4-Methylenedioxymethamphetamine (MDMA, ' ecstasy' ) is re-emerging in clinical settings as a candidate for the treatment of specific psychiatric disorders (e.g. post-traumatic stress disorder) in combination with psychotherapy. MDMA is a psychoactive drug, typically regarded as an empathogen or entactogen, which leads to transporter-mediated monoamine release. Despite its therapeutic...

Identification of 5-HT2A receptor signaling pathways associated with psychedelic potential.

Nat Commun December 15, 2023 Jason Wallach, Andrew B. Cao, Maggie M. Calkins et al. 153 citations

Abstract Serotonergic psychedelics possess considerable therapeutic potential. Although 5-HT 2A receptor activation mediates psychedelic effects, prototypical psychedelics activate both 5-HT 2A -Gq/11 and β-arrestin2 transducers, making their respective roles unclear. To elucidate this, we develop a series of 5-HT 2A -selective ligands with varying Gq efficacies, including β-arrestin-biased...

Identification of 5-HT 2A Receptor Signaling Pathways Responsible for Psychedelic Potential

bioRxiv (Cold Spring Harbor Laboratory) July 31, 2023 Jason Wallach, Andrew B. Cao, Maggie M. Calkins et al. 11 citations preprint

Summary Serotonergic psychedelics possess considerable therapeutic potential. Although 5-HT 2A receptor activation mediates psychedelic effects, prototypical psychedelics activate both 5-HT 2A -Gq/11 and β-arrestin2 signaling, making their respective roles unclear. To elucidate this, we developed a series of 5-HT 2A -selective ligands with varying Gq efficacies, including β-arrestin-biased...

Pharmacological Mechanism of the Non-hallucinogenic 5-HT2A Agonist Ariadne and Analogs

ACS Chemical Neuroscience December 15, 2022 Michael J. Cunningham, Hailey A. Bock, Inis C. Serrano et al. 65 citations

Ariadne is a non-hallucinogenic analog in the phenylalkylamine chemical class of psychedelics that is closely related to an established synthetic hallucinogen, 2,5-dimethoxy-4-methyl-amphetamine (DOM), differing only by one methylene group in the α-position to the amine. Ariadne has been tested in humans including clinical trials at Bristol-Myers Company that indicate a lack of hallucinogenic...