Produtos naturais alucinógenos constituem um importante e interessante grupo de substâncias, em especial os alcaloides, classe de substâncias para as quais são observadas inúmeras atividades biológicas e farmacológicas, incluindo as propriedades alucinógenas apresentadas por várias espécies vegetais que contêm tais metabólitos. Reconhecendo-se a importância histórica, química e farmacológica...
Although psychostimulants apparently do cross the BBB, it is poorly understood how these hydrophilic and positively charged molecules can pass the blood-brain barrier (BBB). That may be mediated by a genetically still uncharacterized H+/OC antiporter with high activity at the BBB. We studied the uptake of 16 psychostimulants and hallucinogens with hCMEC/D3 cells using the prototypic inhibitor...
Abstract Treatment of major depressive disorder (MDD) including treatment-resistant depression (TRD) remains a major unmet need. Although there are several classes of dissimilar antidepressant drugs approved for MDD, the current drugs have either limited efficacy or are associated with undesirable side effects and withdrawal symptoms. The efficacy and side effects of antidepressant drugs are...
There is an increasing interest in the neural effects of psychoactive drugs, in particular tryptamine psychedelics, which has been incremented by the proposal that they have potential therapeutic benefits, based on their molecular mimicry of serotonin. It is widely believed that they act mainly through 5HT2A receptors but their effects on neural activation of distinct brain systems are not...
The emerging therapeutic efficacy of ketamine and classical psychedelics for depression has inspired tremendous interest in the underlying neurobiological mechanisms. We review preclinical and clinical evidence supporting neuroplasticity as a convergent downstream mechanism of action for these novel fast-acting antidepressants. Through their primary glutamate or serotonin receptor targets,...
Abstract. After decades of stagnation, research on psychedelic substances (such as lysergic acid diethylamide [LSD], psilocybin, or N,N-dimethyltryptamine [DMT]) has experienced a renaissance over the last 10 years, with various major research programs being conducted across Europe and the United States. This research primarily investigates the potential of psychedelics in the treatment of...
Background: Serotonergic psychedelics (SPs) like LSD, psilocybin, DMT, and mescaline are a heterogeneous group of substances that share agonism at 5-HT 2a receptors. Besides the ability of these substances to facilitate profoundly altered states of consciousness, persisting psychological effects have been reported after single administrations, which outlast the acute psychedelic effects. In...
Psychedelic drugs (also called hallucinogens, psychotogenics, psycholytics, entheogens) are substances that act mainly on the 5-HT2 serotonergic receptor.There are two main groups of psychedelics: indoleamines (lysergic acid diethylamide-LSD, N, N-dimethyltryptamine-DMT, and psilocybin) and phenethylamines (mescaline, dimethoxymethamphetamine-DOM, methylenedioxyamphetamine-MDA, and...
Ayahuasca is a psychoactive beverage that contains the psychoactive compound N,N-dimethyltryptamine and β-carboline alkaloids. This study aims at determining in vitro the bioavailability and bioaccessibility of the main compounds present in decoctions of four individual plants, in a commercial mixture and in four mixtures of two individual plants used in the preparation of Ayahuasca. The...
Clinical studies suggest the therapeutic potential of psychedelics, including ayahuasca, DMT, psilocybin, and LSD, in stress-related disorders. These substances induce cognitive, antidepressant, anxiolytic, and antiaddictive effects suggested to arise from biological changes similar to conventional antidepressants or the rapid-acting substance ketamine. The proposed route is by inducing brain...