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...
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...
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...
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...
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,...
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, 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...
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...
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...
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.
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,...
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...
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...
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...
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,...
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...
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...
Provided herein are MDMA and their analogs for the potential psychotherapy-assisted treatment of alcohol use disorder (AUD), post-traumatic stress disorder (PTSD), and a method of predicting dosing and patient response.
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, 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....
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...
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,...
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....
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...
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...