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ACS Medicinal Chemistry Letters

ISSN 1948-5875

37 papers in the library · 131 citations · publishing 2020-2026

Papers

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Advancements in Psychoactive Alkaloid Delivery, Neuroenhancement, and Psychedelic Therapies: Exploring the Frontiers of Modern Pharmacology

ACS Medicinal Chemistry Letters May 8, 2024 Robert B. Kargbo 2 citations

This Patent Highlight explores advancements in pharmacology, focusing on the novel delivery and application of psychoactive substances. It highlights the development of transdermal formulations for psychoactive alkaloids, neuroenhancement techniques to augment emotional responses, and the intravenous infusion of psilocybin or psilocin for various therapeutic purposes. Additionally, it delves...

Pioneering Methods in Brain Optimization and Mental Health Treatment.

ACS Medicinal Chemistry Letters March 14, 2024 Robert B. Kargbo

This Patent Highlight explores ground-breaking advancements in neurostimulation, psychedelic therapy, and brain function optimization from recent innovations. It examines methods for altering brain states through AI-driven non-invasive neurostimulation, potentially contributing to personalized brain therapy. The publication also delves into the therapeutic potential of N-isopropyl tryptamines...

Evaluation of the Indazole Analogs of 5-MeO-DMT and Related Tryptamines as Serotonin Receptor 2 Agonists.

ACS Medicinal Chemistry Letters February 8, 2024 Navoda Jayakodiarachchi, Mallory A Maurer, Daniel C Schultz et al. 6 citations

Herein, we report the synthesis and characterization of a novel set of substituted indazole-ethanamines and indazole-tetrahydropyridines as potent serotonin receptor subtype 2 (5-HT2) agonists. Specifically, we examine the 5-HT2 pharmacology of the direct indazole analogs of 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) and related serotonergic tryptamines, and highlight the need for rigorous...

Perceptual Modifying Compounds and Their Potential Therapeutic Applications in Neuropsychiatric Disorders.

ACS Medicinal Chemistry Letters January 11, 2024 Robert B. Kargbo 1 citation

Psychedelic compounds, including ketamine and LSD, have gained renewed interest as potential treatments for neuropsychiatric disorders. These compounds act as psychoplastogens, promoting neuronal growth by activating AMPA receptors, TrkB, and mTOR. The prefrontal cortex plays a crucial role in their therapeutic effects through top-down control over brain regions involved in motivation, fear,...

Tryptamines and Mental Health: Activating the 5-HT Receptor for Therapeutic Potential

ACS Medicinal Chemistry Letters September 15, 2023 Robert B. Kargbo 11 citations

Tryptamines, a class of 3-aminoethyl-indoles that activate the serotonin receptor, show potential for novel mental health treatments. The FDA has granted "breakthrough therapy designation" to psilocybin and MDMA for treatment-resistant depression, major depressive disorder, and post-traumatic stress disorder, sparking global research efforts. Various clinical trials are currently investigating...

Discovery and In Vitro Characterization of SPL028: Deuterated N,N-Dimethyltryptamine.

ACS Medicinal Chemistry Letters September 14, 2023 Marie Layzell, Peter Rands, Meghan Good et al. 6 citations

The psychedelic N,N- dimethyltryptamine (DMT) is in clinical development for the treatment of major depressive disorder. However, when administered via intravenous infusion, its effects are short-lived due to rapid clearance. Here we describe the synthesis of deuterated analogues of DMT with the aim of prolonging the half-life and decreasing the clearance rate while maintaining similar...

Psychoplastogens: A Novel Therapeutic Approach for Neurological Diseases and Disorders.

ACS Medicinal Chemistry Letters September 14, 2023 Robert B. Kargbo 3 citations

Neurological diseases often involve changes in synaptic connectivity and plasticity. Psychoplastogens, substances that stimulate neuronal growth and enhance neural structures, show promise in mitigating these changes. They activate key biological targets, including AMPA receptors, TrkB, and mTOR. Substances like ketamine, scopolamine, N,N-dimethyltryptamine, and rapastinel have...

Subhallucinogenic Concentrations of Substituted Phenethylamines as a Novel Therapeutic Approach for Inflammatory and Neurological Disorders.

ACS Medicinal Chemistry Letters July 13, 2023 Robert B. Kargbo 2 citations

This Patent Highlight presents a method to treat inflammatory or neurological disorders in subjects needing treatment. The method involves administering a therapeutically effective amount of a composition containing a subhallucinogenic concentration of substituted phenethylamine. The substituted phenethylamine may belong to the 2C-X family, including 2C-H, 2C-I, 2C-B, or 2C-E. The specific...

Microbiome–Gut–Brain Axis Modulation: New Approaches in Treatment of Neuropsychological and Gastrointestinal Functional Disorders

ACS Medicinal Chemistry Letters May 11, 2023 Robert B. Kargbo 15 citations

The gut-brain axis (GBA) refers to the sophisticated bidirectional communication system connecting the digestive system with the central nervous system. This interaction is enabled by a series of intricate signaling processes, encompassing various neuro-immune and hormonal pathways. The association between the gut microbiome and mental health has garnered immense scientific and public interest,...

Orally Active Forms of DMT, 5-MeO-DMT, and Long-Acting MDMA for the Treatment of Neuropsychiatric Disorders.

ACS Medicinal Chemistry Letters April 13, 2023 Robert B. Kargbo 4 citations

This Patent Highlight describes derivatives of DMT, 5-MeO-DMT, and MDMA that are metabolically converted to biologically active analogs. When these prodrugs are administered to a subject, they potentially could be used therapeutically in conditions associated with neurological diseases. Furthermore, the disclosure provides methods to potentially treat conditions comprising major depressive...

5-MeO-DMT: Potential Use of Psychedelic-Induced Experiences in the Treatment of Psychological Disorders

ACS Medicinal Chemistry Letters October 21, 2021 Robert B. Kargbo 15 citations

ADVERTISEMENT RETURN TO ISSUEPREVPatent HighlightNEXT5-MeO-DMT: Potential Use of Psychedelic-Induced Experiences in the Treatment of Psychological DisordersRobert B. Kargbo*Robert B. KargboUsona Institute, 277 Granada Drive, San Luis Obispo, California 93401-7337, United States*Email: [email protected]More by Robert B. Kargbohttps://orcid.org/0000-0002-5539-6343Cite this: ACS Med. Chem. Lett....

Psilocybin Therapeutic Research: The Present and Future Paradigm

ACS Medicinal Chemistry Letters March 2, 2020 Robert B. Kargbo 48 citations

Psilocybin, an active component in "magic mushroom", may have the potential to meet the therapeutic needs for a number of indications without the addictiveness and overdose risk of other mind-altering drugs, such as cocaine, heroin, alcohol, methamphetamine, and so forth. The need for new therapies is urgent because addiction, overdose, and suicide deaths have risen throughout the United States...