ASRI Announces Groundbreaking Discovery: Bifunctional 5-HT2A Antagonist and Sodium Channel Blocker Holds Promise for Bipolar Disorder Treatment

News provided by

Alexander Shulgin Research Institute

May 31, 2024, 10:18 ET

LAFAYETTE, Calif., May 31, 2024 /PRNewswire/ -- The Alexander Shulgin Research Institute (ASRI) has unveiled a groundbreaking discovery in the journal Molecular Pharmacology: the first bifunctional compound that acts as both a 5-HT2A receptor antagonist and a voltage-gated sodium channel blocker. This novel molecule, known as XOB, could revolutionize the treatment landscape for bipolar disorder.

Key Findings:

1. XOB's Dual Mechanism of Action:

ASRI Co-Founder and President, Dr. Nicholas Cozzi, spearheaded the design and synthesis of XOB. His team collaborated with experts from leading institutions, including the University of Michigan-Ann Arbor, Stanford University, Medical College of Wisconsin, Usona Institute, and Promega Corporation.
Lead author Dr. Nicholas Denomme, of the University of Michigan-Ann Arbor and Stanford University, guided and performed electrophysiology studies which revealed that XOB had a blocking effect on voltage-gated sodium channels in cultured cells and neurons.
ASRI and Usona Institute scientists performed essential physical and chemical analyses of XOB, while researchers at the Medical College of Wisconsin and Promega Corporation assessed serotonin receptor binding and functional effects.

2. Potential Impact on Bipolar Disorder Treatment:

Bipolar disorder management often involves a combination of drugs, such as a serotonin receptor antagonist (e.g., quetiapine) and a sodium channel blocker (e.g., lamotrigine).
XOB's unique property lies in its ability to perform both functions simultaneously, at similar drug concentrations.
Dr. Cozzi emphasized that XOB represents a proof-of-concept, opening doors to safer and more effective treatments for this challenging disease.

3. Polypharmacology: A New Paradigm:

XOB exemplifies polypharmacology, wherein a single drug targets multiple disease-related pathways.
This approach recognizes that many disorders have complex genetic origins, necessitating multifaceted therapeutic strategies.

ASRI's discovery of XOB marks a significant milestone in psychiatric pharmacology. The potential to address bipolar disorder with a single, multifunctional compound could transform patient care and improve outcomes. Further research and clinical trials will determine XOB's efficacy and safety profile.

Disclaimer: This press release is for informational purposes only and does not constitute medical advice. Consult a healthcare professional for personalized recommendations.

About ASRI:

Established on Bicycle Day in 2021 by Dr. Nicholas Cozzi, Dr. Paul Daley, and the late Ann Shulgin, ASRI continues the legacy of the esteemed chemist Alexander Shulgin, renowned for his pioneering work in discovering psychedelic compounds.

At the forefront of the burgeoning interest in the potential therapeutic benefits of psychedelics, ASRI remains steadfast in its commitment to applied therapeutics, targeting neurological, neurodevelopmental, neuropsychiatric, pain syndrome, inflammation, and overall wellness enhancement domains. Drawing upon a wealth of knowledge in chemistry, pharmacology, and neuroscience, ASRI is committed to catalyzing positive change in global healthcare. Noteworthy is the Shulgin Vault, housing an extensive repository of over 500 compounds synthesized by Alexander "Sasha" Shulgin and ASRI scientists, offering a rich spectrum of novel variations spanning phenylalkylamines, tryptamines, lysergamides, isoquinolines, cathinones, and more. For more information on ASRI, please visit: www.ShulginResearch.net.

Forward-looking statement:

This release contains forward-looking statements regarding ASRI's anticipated future events and outcomes, such as data projections and advancements in drug discovery methods. These statements are based on current expectations and assessments but are subject to various risks and uncertainties. Factors such as the ongoing impact of COVID-19, fluctuations in economic conditions, market dynamics, regulatory constraints, and other variables may cause actual results to differ from those anticipated. While ASRI's management has made reasonable assumptions, the actual outcomes may deviate significantly. It's important to note that ASRI has refrained from making medical assertions about its products, and regulatory bodies like the FDA have not yet evaluated their effectiveness. Rigorous clinical trials are necessary for validation, a process which ASRI has not yet undertaken. Without obtaining the required approvals or conducting essential research, ASRI's performance and operations may be negatively impacted. Therefore, stakeholders should be mindful of these uncertainties when considering the forward-looking statements contained in this release.‍

Media Contact:
Kathy Lanser,
[email protected]

SOURCE Alexander Shulgin Research Institute