Robert B. Kargbo - The Consciousness Library

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...

DOI: 10.1021/acsmedchemlett.3c00309 Full text Brain plasticity Mental health Psychopharmacology Therapeutic research

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

ACS Med Chem Lett 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.

DOI: 10.1021/acsmedchemlett.3c00333 Full text Psychedelic therapy Mental health Personalized medicine Medical innovation +1

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 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 Full text Novel therapeutics Sub-hallucinogenic dosing Phenethylamine compounds Chronic disease treatment

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 Full text 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 Full text Psychedelics Mental health treatment Drug development Therapeutic compounds

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 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...

DOI: 10.1107/s2053229621013164 Full text

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....

DOI: 10.1021/acsmedchemlett.1c00546 Full text Psychotherapist Clinical psychology

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...

DOI: 10.1021/acs.jnatprod.1c00087 Full text Psilocybin Tryptamine Biological activity Biochemistry +3

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 Psilocybin Natural product Tryptophan Biochemistry +4

Direct Phosphorylation of Psilocin Enables Optimized cGMP Kilogram-Scale Manufacture of Psilocybin

ACS Omega July 1, 2020 Jessica Sable, Tura Patterson, Gary Tarpley et al. 41 citations

A second-generation kilogram-scale synthesis of the psychedelic tryptamine psilocybin has been developed. The synthesis was designed to address several challenges first encountered with the scale-up of previously described literature procedures, which were not optimized for providing consistent yield and purity of products, atom economy, or being run in pilot plant-scale reactors. These...

DOI: 10.1021/acsomega.0c02387 Psilocybin Phosphorylation

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...

DOI: 10.1021/acsmedchemlett.0c00048 Full text Psilocybin Data science

Scalable Hybrid Synthetic/Biocatalytic Route to Psilocybin

Chemistry - A European Journal February 26, 2020 Janis Fricke, Robert B. Kargbo, Lars Regestein et al. 48 citations

Abstract Psilocybin, the principal indole alkaloid of Psilocybe mushrooms, is currently undergoing clinical trials as a medication against treatment‐resistant depression and major depressive disorder. The psilocybin supply for pharmaceutical purposes is met by synthetic chemistry. We replaced the problematic phosphorylation step during synthesis with the mushroom kinase PsiK. This enzyme was...

DOI: 10.1002/chem.202000134 Psilocybin Tryptamine Combinatorial chemistry Pharmacology +3

Synthesis and Biological Evaluation of Tryptamines Found in Hallucinogenic Mushrooms: Norbaeocystin, Baeocystin, Norpsilocin, and Aeruginascin

Journal of Natural Products February 20, 2020 Alexander M. Sherwood, Adam L. Halberstadt, Adam K. Klein et al. 79 citations

A general synthetic method was developed to access known tryptamine natural products present in psilocybin-producing mushrooms. In vitro and in vivo experiments were then conducted to inform speculations on the psychoactive properties, or lack thereof, of the natural products. In animal models, psychedelic activity by baeocystin alone was not evident using the mouse head twitch response assay,...

DOI: 10.1021/acs.jnatprod.9b01061 Psilocybin Tryptamines Hallucinogen Metabolite +11

An Improved, Practical, and Scalable Five-Step Synthesis of Psilocybin

Synthesis January 8, 2020 Robert B. Kargbo, Alexander M. Sherwood, Poncho Meisenheimer et al. 31 citations

Described herein is an improved synthesis of 3-[2-(dimethylamino)ethyl]-1H-indol-4-yl dihydrogen phosphate (psilocybin). The protocol outlines: synthesis of multigram quantities of psilocybin, identification of critical in-process parameters, and isolation of psilocybin without the use of chromatography, TLC, or aqueous workup. The synthesis furnishes psilocybin in five steps in 23% overall...

DOI: 10.1055/s-0039-1691565 Full text Psilocybin Yield engineering Combinatorial chemistry Hallucinogen +2

Enzymatic Route toward 6‐Methylated Baeocystin and Psilocybin

ChemBioChem May 31, 2019 Janis Fricke, Alexander M. Sherwood, Robert B. Kargbo et al. 38 citations

Abstract Psilocybin and its direct precursor baeocystin are indole alkaloids of psychotropic Psilocybe mushrooms. The pharmaceutical interest in psilocybin as a treatment option against depression and anxiety is currently being investigated in advanced clinical trials. Here, we report a biocatalytic route to synthesize 6‐methylated psilocybin and baeocystin from 4‐hydroxy‐6‐methyl‐ l...

DOI: 10.1002/cbic.201900358 Psilocybin Enzyme Indole test Methylation +6

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