ACS Medicinal Chemistry Letters
July 10, 2026
Anna C. Renner, Robert B. Kargbo
High Resolution Image Download MS PowerPoint Slide The psychedelic therapeutics field continues to evolve beyond classical hallucinogens toward integrated treatment platforms that combine optimized pharmacology, drug delivery, and clinical implementation. Recent patent applications disclose selective 5-HT2A receptor activators, precision aerosol delivery technologies for psychedelic compounds,...
ACS Medicinal Chemistry Letters
December 16, 2025
Anna C. Renner, Robert B. Kargbo
Emerging psychedelic therapeutics increasingly rely on mechanistic precision, receptor selectivity, and pharmacokinetic control. Recent inventions introduce simplified iboga analogs with tunable polypharmacology, real-time EEG biomarkers that individualize psilocybin dosing, and standardized harmine-DMT ratios with high bioavailability. Together, these innovations form a coherent framework for...
ACS Medicinal Chemistry Letters
December 16, 2025
Anna C. Renner, Robert B. Kargbo
New inventions introduce complementary advances across neuropsychiatric therapeutics: a blood-based gene-expression diagnostic centered on FOXG1 for objective PTSD detection; benzocyclobutenyl-methylamine modulators that normalize neuronal hyperexcitability; and templated-carrier sublingual 5-MeO-DMT formulations enabling controlled, nonhallucinogenic neuroplasticity. Together, these approaches...
ACS Medicinal Chemistry Letters
October 10, 2025
Anna C. Renner, Robert B. Kargbo
A crystalline cocrystal of psilocin and psilocybin enhances exposure, neuroplasticity biomarkers, and functional activity, while adjunctive atypical antipsychotics modulate serotonergic signaling to mitigate 5-HT2B-linked safety concerns. Together, these inventions advance formulation, mechanistic selectivity, and translational biomarkersoffering a chemistry-enabled path to scalable...
ACS Medicinal Chemistry Letters
August 15, 2025
Robert B. Kargbo
Novel phenalkylamines and tryptamines such as psilocybin demonstrate promising nontraditional pharmacological profiles for treating psychiatric syndromes. Structural modifications yield functional selectivity at 5-HT receptors, mitigating hallucinogenic risk while preserving therapeutic efficacy. This study integrates receptor and behavioral data to support phenalkylamines and psilocybin as...
Journal of Labelled Compounds and Radiopharmaceuticals
July 1, 2025
Rodney D. Brown, Niall M. Hamilton, Connor Mallon et al.
1 citation
ABSTRACT Three novel 14 C‐labelled isotopologues of the psychoactive agents psilocin, psilocybin and 5‐methoxy‐ N , N ‐dimethyltryptamine (5‐MeO‐DMT) were synthesised, all labelled at the 2‐position of the indole. The syntheses involved incorporating the 3‐dimethylaminoethyl substituent common to all three substances onto a 4‐ or 5‐substituted indole intermediate via successive treatments with...
ACS Medicinal Chemistry Letters
June 12, 2025
Robert B. Kargbo
1 citation
Innovative formulations of N,N-dimethyltryptamine (DMT) and 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) enable parenteral and intranasal delivery, respectively. These delivery systems overcome limitations of poor bioavailability and rapid metabolism, offering rapid-onset, short-duration therapeutic effects. The compositions support controlled psychedelic interventions for psychiatric...
ACS Medicinal Chemistry Letters
June 12, 2025
Robert B. Kargbo
Substituted tryptamines with selective 5-HT2A/2C activity demonstrate therapeutic promise without psychedelic effects. Two recent patent applications describe nonhallucinogenic analogs for metabolic and neuropsychiatric disorders. These agents exhibit optimized receptor selectivity, metabolic synergy, and neuroplastic potential, offering a novel chemical framework for multimodal treatment...
ACS Medicinal Chemistry Letters
May 8, 2025
Robert B. Kargbo
1 citation
DMT induces rapid antidepressant effects, but acute sympathomimetic side effects, particularly hypertension and tachycardia, limit its use. This study describes coformulations with short-acting beta-blockers or nitrates, matched to DMT's pharmacokinetics, to mitigate peripheral cardiovascular risks without compromising central therapeutic action, facilitating safer psychedelic therapy in...
ACS Medicinal Chemistry Letters
April 10, 2025
Robert B. Kargbo
Psilocybin demonstrates a clinically meaningful reduction in phantom and residual limb pain. Adaptive sensory environments (ASEs) separately offer biosensor-guided modulation of psychological states during psychoactive therapy. This Patent Highlight explores the pharmacological findings of a psilocybin trial and discusses future integration with ASE systems to precision and scale...
ACS Medicinal Chemistry Letters
April 10, 2025
Robert B. Kargbo
Recent advancements in psychedelic therapeutics, tryptamine derivatives, neuroplastic modulators, and AI-powered machine-learning platforms mark a new frontier in precision medicine. These innovations address critical challenges in neurological and psychiatric disorders, chronic pain management, and computational accessibility. By harnessing the principles of receptor modulation, targeted...
ACS Medicinal Chemistry Letters
April 10, 2025
Robert B. Kargbo
Psychedelics and AI modulate cognitive frameworks, disrupt rigid thought patterns, and enhance neuroplasticity, offering therapeutic potential for depression, PTSD, and addiction. Relaxing neural filters reveal altered states of consciousness, challenging perceptions of reality. This Viewpoint explores their neurobiological mechanisms and AI's role in augmenting psychiatric treatments.
ACS Medicinal Chemistry Letters
February 13, 2025
Robert B. Kargbo
Integrating advanced pharmaceutical innovations and artificial intelligence (AI) offers transformative potential for psychiatric care. This Patent Highlight reviews novel therapeutic strategies, including the synergistic use of monoamine antidepressants and short-duration psychedelics, alongside AI-driven behavioral efficacy tracking. The combination of selective serotonin reuptake inhibitors...
ACS Medicinal Chemistry Letters
January 9, 2025
Robert B. Kargbo
Artificial intelligence (AI) offers transformative potential in psychedelic research by addressing limitations in personalized treatment, predicting therapeutic outcomes, and understanding complex biological and environmental factors. AI-driven models provide new insights into long-term efficacy, set and setting optimization, and alternative treatment methods, advancing psychedelic therapy into...
ACS Medicinal Chemistry Letters
December 12, 2024
Robert B. Kargbo
Psychedelic compounds, particularly psilocybin and psilocin, have shown significant therapeutic potential in treating neurological and psychiatric disorders. However, their bioavailability, rapid metabolism, and stability challenges have limited their clinical use. This Patent Highlight reviews recent innovations in psychedelic drug delivery systems and the development of psilocin analogs aimed...
ACS Medicinal Chemistry Letters
November 14, 2024
Robert B. Kargbo
3 citations
Recent advancements in the therapeutic use of psychedelic compounds, particularly 5-MeO-DMT and DMT, have demonstrated significant potential in treating various mental health disorders. This Patent Highlight evaluates findings from multiple recent patents that explore novel applications of these compounds, including their use in severe psychiatric conditions such as depression, anxiety, and...
ACS Med Chem Lett
November 11, 2024
Robert B. Kargbo
High Resolution Image Download MS PowerPoint Slide Recent innovations in psychedelic research have led to the development of novel compounds designed to enhance the therapeutic potential of psilocin and related tryptamines. This Patent Highlight reviews three essential patents that focus on improving the stability, bioavailability, and efficacy of these compounds for treating mental health...
ACS Medicinal Chemistry Letters
October 15, 2024
Robert B. Kargbo
1 citation
Psilocybin, a naturally occurring psychedelic compound, has recently emerged as a promising therapeutic agent for mental health. This Patent Highlight explores the innovative approaches to harnessing psilocybin's potential across various contexts. These include clinical trials targeting severe psychiatric conditions, the integration of low-dose psilocybin into dietary products to promote...
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...
ACS Medicinal Chemistry Letters
August 21, 2024
Robert B. Kargbo
Recent advancements in medical research have focused on the utilization of entheogens, particularly psilocybin and its related compounds, as therapeutic agents in mitigating cognitive decline and enhancing psychological resilience in patients undergoing anesthesia and sedation. This Patent Highlight integrates findings from three patent applications, each contributing unique insights into the...
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...
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...
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...
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,...
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...