Provided herein are novel 3-pyrrolidineindole derivatives as serotonergic psychedelic agents, pharmaceutical compositions, use of such compounds in treating psychosis and mental illnesses such as depression and post-traumatic stress disorder, and processes for preparing such compounds.
Recent advancements in the study of mushroom-derived tryptamines, particularly psilocybin and its metabolite psilocin, highlight their unique psychedelic properties and potential therapeutic applications, especially for mental health conditions like depression. This study examines how the position of the hydroxyl group on the indole ring affects the 5-HT2A receptor activity and psychedelic-like...
Provided herein are novel 3-cycloaminoindole compounds as serotonergic psychedelic agents, pharmaceutical compositions, use of such compounds in treating psychosis, mental illness and central nervous system (CNS) disorders and processes for preparing such compounds.
Book of Proceedings2025Marina D. Kostić, Jana Nedić, Jovana S. Dragojević et al.
Serotonin receptors, also known as 5-hydroxytryptamine (5-HT) receptors, are a diverse family of G protein-coupled and ligand-gated ion channel receptors that mediate the physiological effects of the neurotransmitter serotonin. These receptors are widely distributed throughout the central and peripheral nervous systems, where they regulate numerous processes including mood, cognition,...
Research2025Shujie Li, Shu-Jie Li, Qingning Yuan et al.
The 5-HT 1A receptor is a critical target in the treatment of depression and anxiety. Bufotenine derivatives, such as 5-methoxy- N , N -dimethyltryptamine (5-MeO-DMT), 5-hydroxy- N , N -dimethyltryptamine (5-OH-DMT), and 5-hydroxy- N , N , N -dimethyltryptamine—derived from traditional Chinese medicine—have shown antidepressant potential. However, the structural basis of their interaction with...
Psychedelics are primarily recognized for their profound behavioral effects, leading most research on psychedelics and their primary target, the 5-HT2A receptor, to focus on brain activity. However, these receptors are not only found within the brain and are present in nearly every tissue and cell type throughout the body, playing a significant role alongside serotonin in modulating various...
Depressive disorders continue to pose a major clinical challenge worldwide, particularly given the high prevalence and increasing number of treatment-resistant cases. Over the past decade, advances in research have elucidated the antidepressant potential of psilocybin and other 5-HT₂A receptor agonists in patients with major depressive disorder (MDD) and treatment-resistant depression (TRD)....
Silene undulata is historically used for inducing vivid and prophetic lucid dreams, but limited information exists on its phytochemical composition and potential pharmacological properties. This study aimed to investigate the phytochemical composition of S. undulata through LC-MS/MS analysis and explore its potential serotonergic activity, which could support and confirm the traditional use of...
Serotonergic psychedelics have potential therapeutic effects in treating anxiety and mood disorders, often after a single dose, and are suggested to have plasticity-inducing action. However, a comprehensive mechanism of action is still lacking. Here, we investigated how a single dose of the short-acting 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) acts on gene expression from microdissected...
5-methoxy-N,N-dimethyltrytpamine (5-MeO-DMT) analogs are used as recreational drugs, but they are also being developed as potential medicines, warranting further investigation into their pharmacology. Here, we investigated the neuropharmacology of 5-MeO-DMT and several of its N-alkyl, N-allyl, and 2-methyl analogs, with three major aims: 1) to determine in vitro receptor profiles for the...