Six-Step Synthesis of (?)-Lysergic Acid

Article Multidisciplinary Sciences

Structure-based discovery of nonhallucinogenic psychedelic analogs

Dongmei Cao et al.

Summary: This study provides structural insights into the binding of drugs to 5-HT2AR and offers a foundation for the design of safe and effective nonhallucinogenic psychedelic analogs for the treatment of neuropsychiatric diseases.

SCIENCE (2022)

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Article Chemistry, Organic

A Short Synthesis of Ergot Alkaloids and Evaluation of the 5-HT1/2 Receptor Selectivity of Lysergols and Isolysergols

Nikhil R. Tasker et al.

Summary: This study describes the total synthesis of ergot alkaloids, including the previously unknown stereoisomers, using key transformations and streamlined experimental procedures. The synthesized compounds can be used for pharmacological evaluation.

ORGANIC LETTERS (2022)

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Article Multidisciplinary Sciences

A non-hallucinogenic psychedelic analogue with therapeutic potential

Lindsay P. Cameron et al.

Summary: The study identifies key structural elements of the potential therapeutic pharmacophore of ibogaine and designs tabernanthalog, a safer, non-hallucinogenic analogue of ibogaine. Tabernanthalog is found to promote neural plasticity, reduce addiction-related behavior, and produce antidepressant effects in rodents. Through careful chemical design, it is possible to modify psychedelic compounds to produce safer, non-hallucinogenic variants with therapeutic potential.

NATURE (2021)

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Article Chemistry, Organic

Asymmetric Synthesis of Lysergic Acid via an Intramolecular (3+2) Dipolar Cycloaddition/Ring-Expansion Sequence

Upendra Rathnayake et al.

Summary: An effective and potentially scalable asymmetric synthesis of lysergic acid, a core component of the ergot alkaloid family, was reported. The synthesis involved intramolecular azomethine ylide cycloaddition and Cossy-Charette ring expansion to assemble the target compound's C- and D-rings. The strategy allowed for the preparation of novel ergot analogues, including unnatural antipodes, and offered a more amenable approach to analogue generation compared to previous methods.

ORGANIC LETTERS (2021)

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Article Chemistry, Medicinal

Combining Psychedelic and Mindfulness Interventions: Synergies to Inform Clinical Practice

Jake E. Payne et al.

Summary: Psychedelic and mindfulness interventions have shown to improve mental health and wellbeing, but they also have specific challenges. The authors propose combining these two interventions for greater benefit, with psychedelic treatments initiating and motivating while mindfulness interventions integrating and maintaining the effects. Testable hypotheses and future research are outlined regarding the synergistic action of these interventions for improved clinical outcomes.

ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE (2021)

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Article Chemistry, Multidisciplinary

A predictive model for additions to N-alkyl pyridiniums

Brian J. Knight et al.

Summary: This study presents a comprehensive investigation into the dearomative addition of organomagnesium nucleophiles to N-alkyl pyridinium electrophiles, revealing observable and predictable regiochemical outcomes associated with substituent patterns. The effects of substituents on the pyridinium electrophile can be either additive or ablative, affecting the selectivity of the reaction. Additionally, the nature of the organometallic nucleophilic component plays a significant role in determining the regioselective outcome of the reaction.

CHEMICAL COMMUNICATIONS (2021)

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Article Chemistry, Medicinal

The Subjective Effects of Psychedelics May Not Be Necessary for Their Enduring Therapeutic Effects

David E. Olson

Summary: Psychedelics have shown promise for treating neuropsychiatric disorders due to their ability to promote neural plasticity and produce rapid and sustained therapeutic effects, but evidence suggests that the subjective effects induced by these drugs may not be necessary for long-lasting changes in mood and behavior. Understanding the role of subjective effects in the therapeutic mechanisms of psychedelics will have important implications for basic neuroscience and patient access to future medicines developed from psychedelic research.

ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE (2021)

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Article Chemistry, Medicinal