Correlation of psychotomimetic activity of phenethylamines and amphetamines with 1-octanol-water partition coefficients. Serotonin in the gut: blessing or a curse. Molecular basis of partial agonism: orientation of indoleamine ligands in the binding pocket of the human serotonin 5-HT 2A receptor determines relative efficacy. 11C labeling of indolealkylamine alkaloids and the comparative-study of their tissue distributions. Moving beyond rules: the development of a central nervous system multiparameter optimization (CNS MPO) approach to enable alignment of druglike properties. A ‘rule of three’ for fragment-based lead discovery? Drug Discov. Comparative effects of stereoisomers of psychotomimetic phenylisopropylamines. Indolealkylamine and phenalkylamine hallucinogens-effect of α-methyl and N-methyl substituents on behavioral activity. Inhibition of monoamine oxidase by amphetamine and related compounds. Comparison of the behavioral responses induced by phenylalkylamine hallucinogens and their tetrahydrobenzodifuran (‘FLY’) and benzodifuran (‘DragonFLY’) analogs. 1-Aminomethylbenzocycloalkanes: conformationally restricted hallucinogenic phenethylamine analogues as functionally selective 5-HT 2A receptor agonists. Indolealkylamine analogs share 5-HT 2 binding characteristics with phenylalkylamine hallucinogens. Serotonin receptor-binding affinities of several hallucinogenic phenylalkylamine and N, N-dimethyltryptamine analogs. Psychedelic-inspired drug discovery using an engineered biosensor. Gramine: a vasorelaxing alkaloid acting on 5-HT 2A receptors. Structure-based discovery of nonhallucinogenic psychedelic analogs. Structure of a hallucinogen-activated Gq-coupled 5-HT 2A serotonin receptor. The promises and perils of psychedelic pharmacology for psychiatry. Psychedelic drugs: neurobiology and potential for treatment of psychiatric disorders. Long-term follow-up of psilocybin-facilitated smoking cessation.
FANTAVISION PSYCHIDELIC EFFECT TRIAL
Trial of psilocybin versus escitalopram for depression.
Effects of psilocybin-assisted therapy on major depressive disorder: a randomized clinical trial.
The history of psychedelics in psychiatry. By synthesizing knowledge across the chemical, molecular, neuronal, and network levels, we hope to provide an integrative perspective on the neural mechanisms responsible for the acute and enduring effects of psychedelics on behavior. Finally, we summarize neuroimaging results that pinpoint effects on association cortices and thalamocortical functional connectivity, which inform current theories of psychedelic action. We consider the impact of psychedelics on neuronal spiking dynamics in several cortical and subcortical regions, along with transcriptional changes and sustained effects on structural plasticity. We describe the roles of serotonin receptors and their downstream molecular signaling pathways, emphasizing key elements for drug discovery. We first discuss chemistry, highlighting the diversity of psychoactive molecules and the principles that govern their potency and pharmacokinetics. In this review, we focus on the basic neurobiology underlying the action of psychedelic drugs. Psychedelics are serotonin 2A receptor agonists that can lead to profound changes in perception, cognition and mood.
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