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Robert B. Kargbo

Usona Institute

56 papers in the library · 431 citations · publishing 2019-2026

Papers

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Current Trends in Psychedelic Science: Integrating Modified Lysergic Acid Derivatives and Psilocybin in Modern Medicine

ACS Medicinal Chemistry Letters August 21, 2024 Robert B. Kargbo

This article explores groundbreaking advancements in psychedelic research, highlighting the development of novel lysergic acid derivatives with modified LSD-like actions and innovative dosing methods based on ABCF1 gene expression for psilocybin. It also examines new strategies for treating binge eating disorder using psychedelics and techniques for neuroenhancement to enhance emotional...

Innovative Ketamine Formulations: Enhancing Therapeutic Efficacy and Safety.

ACS Medicinal Chemistry Letters August 8, 2024 Robert B. Kargbo 1 citation

Ketamine, originally developed as an anesthetic, has shown significant potential for treating depression, chronic pain, and other conditions. However, its conventional formulations often result in side effects such as hallucinations and dizziness due to rapid spikes in blood concentration. This article explores recent patents that optimize ketamine delivery and efficacy: subcutaneous injectable...

DOI: 10.1021/acsmedchemlett.4c00330 (opens in new tab) Full text (opens in new tab) Ketamine-therapy Drug-delivery-systems Pharmaceutical-innovation Depression-treatment

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...

DOI: 10.1021/acsmedchemlett.4c00181 (opens in new tab) Psilocybin Transdermal Pharmacology Neurostimulation +2

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...

DOI: 10.1021/acsmedchemlett.4c00058 (opens in new tab) Full text (opens in new tab) Psychedelics Artificial intelligence Brain stimulation Mental health

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,...

DOI: 10.1021/acsmedchemlett.3c00535 (opens in new tab) Full text (opens in new tab) Psychedelics Mental-health Brain-plasticity Therapeutic-medicine

Small-Molecule Heterocyclic Compounds: Gq-Biased Agonists for the 5-HT2A Receptor in Neuropsychiatric Treatment

ACS Medicinal Chemistry Letters October 19, 2023 Robert B. Kargbo 2 citations

Addressing the significant challenges of treating depression, anxiety, and substance abuse, this Patent Highlight explores the development of innovative small-molecule heterocyclic compounds as Gq-biased agonists of the 5-HT2A receptor. Unlike traditional treatments, these compounds selectively activate 5-HT2A-mediated Gq signaling, excluding related receptors like 5-HT2B and 5-HT2C. This...

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...

DOI: 10.1021/acsmedchemlett.3c00390 (opens in new tab) Full text (opens in new tab) Tryptamines 5-HT Receptor Pharmacology Data science

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...

Exploring Next-Generation Therapeutics: Morphic Mixtures and Specified Salts for the Treatment of Mental Disorders and CNS Modulation

ACS Medicinal Chemistry Letters August 22, 2023 Robert B. Kargbo

This Patent Highlight delves into the potential of next-generation therapeutics for treating mental disorders and modulating the central nervous system (CNS). Among the serotonin receptor subtypes, 5-HT2A, 5-HT2C, 5-HT1A, and 5-HT1B have shown promise in CNS disorder treatment. Approved drugs targeting these receptors, such as antipsychotics and psychedelics, provide valuable insights into...

Pioneering Changes in Psychiatry: Biomarkers, Psychedelics, and AI.

ACS Medicinal Chemistry Letters August 18, 2023 Robert B. Kargbo 3 citations

This viewpoint discusses integrating biomarkers, psychedelics, and AI into psychiatry for enhanced diagnostics, prognosis, and treatment. It highlights the potential of psychedelics in therapy, AI's role in predicting treatment response, and the challenges that must be addressed. The aim is to encourage research for more precise, personalized psychiatric care.

The Synergistic Effects of 5-HT2A and TRP Agonism/Antagonism in Reducing Inflammation for Enhanced Mental and Physical Health.

ACS Medicinal Chemistry Letters August 10, 2023 Robert B. Kargbo

Depression is a widespread issue in the United States and the leading cause of disability globally, impacting people of all ages. Although selective serotonin reuptake inhibitors (SSRIs) are commonly used for treatment, they have limited effectiveness and may take weeks to show results. There is a pressing need for fast and effective solutions for various types of depression, including chronic,...

Microbiome: The Next Frontier in Psychedelic Renaissance

Journal of Xenobiotics July 25, 2023 Robert B. Kargbo 5 citations

The psychedelic renaissance has reignited interest in the therapeutic potential of psychedelics for mental health and well-being. An emerging area of interest is the potential modulation of psychedelic effects by the gut microbiome—the ecosystem of microorganisms in our digestive tract. This review explores the intersection of the gut microbiome and psychedelic therapy, underlining potential...

DOI: 10.3390/jox13030025 (opens in new tab) Gut microbiome Mental health The renaissance Mood +1

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...

DOI: 10.1021/acsmedchemlett.3c00220 (opens in new tab) Full text (opens in new tab) Novel therapeutics Sub-hallucinogenic dosing Phenethylamine compounds Chronic disease treatment

Unraveling Psychedelic Responses: Targeted Protein Degradation and Genetic Diversity

ACS Medicinal Chemistry Letters July 11, 2023 Robert B. Kargbo

This Viewpoint discusses the intersection of targeted protein degradation (TPD) technologies and psychedelic research. The resurgence in interest in psychedelics for treating mental disorders and the known genetic variability in responses require new strategies. TPD technologies might address this variability, modulating protein expressions based on genetic profiles. The discussion includes...

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,...

DOI: 10.1021/acsmedchemlett.3c00168 (opens in new tab) Full text (opens in new tab) Gut–brain axis Gut microbiome Lysergic acid Enteric nervous system +1

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...

DOI: 10.1021/acsmedchemlett.3c00077 (opens in new tab) Full text (opens in new tab) Psychedelics Mental health treatment Drug development Therapeutic compounds

Psychedelic-Assisted Neuroplasticity for the Treatment of Mental Health Disorders

ACS Medicinal Chemistry Letters January 18, 2023 Robert B. Kargbo 2 citations

The renaissance of research into psychedelics class of drugs has renewed interest for a possible psychedelic clinical therapy for treating psychiatric conditions such as treatment-resistant depression, major depressive-disorder, post-traumatic stress disorder, and other neuropsychiatric diseases. Psychedelics are known to stimulate neurogenesis and gliogenesis, reduce inflammation, and...

Application of Deuterated N,N-Dimethyltryptamine in the Potential Treatment of Psychiatric and Neurological Disorders.

ACS Medicinal Chemistry Letters August 22, 2022 Robert B. Kargbo

ADVERTISEMENT RETURN TO ISSUEPREVPatent HighlightNEXTApplication of Deuterated N,N-Dimethyltryptamine in the Potential Treatment of Psychiatric and Neurological DisordersRobert B. Kargbo*Robert B. KargboUsona Institute, Fitchburg, Wisconsin 53711-5300, United States*E-mail: [email protected]More by Robert B. Kargbohttps://orcid.org/0000-0002-5539-6343Cite this: ACS Med. Chem. Lett. 2022, 13, 9,...

Psilocybin: Characterization of the Metastable Zone Width (MSZW), Control of Anhydrous Polymorphs, and Particle Size Distribution (PSD)

ACS Omega February 7, 2022 Robert B. Kargbo, Alexander M. Sherwood, Poncho Meisenheimer et al. 5 citations

Psilocybin, a serotonergic agonist, was granted a "breakthrough therapy" status by the Food and Drug Administration for clinical trials involving major depressive disorder and treatment-resistant depression. The direct phosphorylation of psilocin to psilocybin that uses a fast crystallization associated with a kinetically controlled process resulted in a smaller particle size distribution....

DOI: 10.1021/acsomega.1c06708 (opens in new tab) Psilocybin Nucleation Metastability Recrystallization geology +7

Psilocybin: crystal structure solutions enable phase analysis of prior art and recently patented examples

Acta Crystallographica Section C Structural Chemistry December 20, 2021 Alexander M. Sherwood, Robert B. Kargbo, Kristi W. Kaylo et al. 10 citations

Psilocybin {systematic name: 3-[2-(dimethylamino)ethyl]-1 H -indol-4-yl dihydrogen phosphate} is a zwitterionic tryptamine natural product found in numerous species of fungi known for their psychoactive properties. Following its structural elucidation and chemical synthesis in 1959, purified synthetic psilocybin has been evaluated in clinical trials and has shown promise in the treatment of...

The Psychedelic Renaissance: Addressing Potential Adverse Effects in a Therapeutic Setting.

ACS Medicinal Chemistry Letters November 8, 2021 Robert B. Kargbo

ADVERTISEMENT RETURN TO ISSUEPREVPatent HighlightNEXTThe Psychedelic Renaissance: Addressing Potential Adverse Effects in a Therapeutic SettingRobert 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. 2021, 12, 12,...

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....

Chemoenzymatic Synthesis of 5-Methylpsilocybin: A Tryptamine with Potential Psychedelic Activity

Journal of Natural Products March 5, 2021 Janis Fricke, Alexander M. Sherwood, Adam L. Halberstadt et al. 18 citations

A novel analogue of psilocybin was produced by hybrid chemoenzymatic synthesis in sufficient quantity to enable bioassay. Utilizing purified 4-hydroxytryptamine kinase from Psilocybe cubensis, chemically synthesized 5-methylpsilocin (2) was enzymatically phosphorylated to provide 5-methylpsilocybin (1). The zwitterionic product was isolated from the enzymatic step with high purity utilizing a...

Taking Different Roads: l‐Tryptophan as the Origin of Psilocybe Natural Products

ChemPlusChem October 1, 2020 Claudius Lenz, Alexander M. Sherwood, Robert B. Kargbo et al. 40 citations

Abstract Psychotropic fungi of the genus Psilocybe , colloquially referred to as „magic mushrooms”, are best known for their l ‐tryptophan‐derived major natural product, psilocybin. Yet, recent research has revealed a more diverse secondary metabolism that originates from this amino acid. In this minireview, the focus is laid on l ‐tryptophan and the various Psilocybe natural products and their...

DOI: 10.1002/cplu.202000581 (opens in new tab) Psilocybin Natural product Tryptophan Biochemistry +4