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Dibenzo- and benzindolo-azecines represent a novel class of high-affinity dopamine receptor antagonists. To further characterize these drugs as potential neuroleptics, we selected a set of azecine derivatives and ring expanded homologues and we measured their antagonist activity at the 5-HT(2A) receptor in the porcine coronary artery. SARs found for the 5-HT(2A) receptor resemble those for the D1 but not the D2 receptor. The protein-ligand interactions were discussed with respect to the different binding pockets.
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http://dx.doi.org/10.1016/j.bmcl.2008.04.081 | DOI Listing |
Importance: Effective and well-tolerated pharmacotherapies for generalized anxiety disorder (GAD), which is one of the most common psychiatric disorders, are needed.
Objective: To determine the dose-response relationship of MM120 (lysergide D-tartrate) in adults with moderate to severe GAD.
Design, Settings, And Participants: This phase 2b, multicenter, randomized, double-blind, placebo-controlled study enrolled 198 adults aged 18 to 74 years with a primary GAD diagnosis who presented with moderate to severe symptoms (defined by a Hamilton Anxiety Rating Scale [HAM-A] score ≥20) and was conducted at 22 outpatient psychiatric research sites in the US from August 2022 to August 2023.
Acta Neuropsychiatr
September 2025
Department of Developmental and Personality Psychology, Laboratory of Experimental Psychology, Neuroscience, and Behavior (LPNeC), Universidade Federal of Rio Grande do Sul (UFRGS), Brazil.
Background: Major depressive disorder (MDD) is a significant public health concern, and current treatments often have limitations in effectiveness and adherence. Psilocybin, a psychedelic compound found in certain mushrooms, is being explored as a potential treatment for depression. It primarily acts through the serotonin 5-HT2A receptor but interacts with 5-HT1A and 5-HT2C receptors.
View Article and Find Full Text PDFZh Nevrol Psikhiatr Im S S Korsakova
August 2025
Russian Medical Academy of Continuing Professional Education, Moscow, Russia.
Objective: To identify pharmacogenetic markers of the effectiveness and safety of sertraline pharmacotherapy at polymorphic loci (-1438G>A, rs6311), (102c>T, rs6313), (1354C/T, rs6314), (rs7997012 G>A) of the gene in patients with mixed anxiety-depressive disorder from the Republic of Bashkortostan.
Material And Methods: The study included 100 patients treated with sertraline. The effectiveness and safety of sertraline therapy in patients were assessed using standardized psychometric scales on the day before the start of therapy and then for 42 days.
Sheng Wu Gong Cheng Xue Bao
August 2025
State Key Laboratory of Chemistry for NBC Hazards Protection, Beijing 102205, China.
The 5-hydroxytryptamine 2A receptor (5-HTR) is one of the key targets in the development of novel antidepressants. To develop new antidepressants targeting the 5-HT receptor, this study established a high-throughput screening method for drugs targeting the 5-HT receptor based on the principle of detecting calcium flux signals. The immunofluorescence assay and western blotting were employed to evaluate receptor expression levels in the 5-HTR-CHO cell line.
View Article and Find Full Text PDFJ Psychopharmacol
August 2025
Otsuka America Pharmaceutical, Inc., Princeton, NJ, USA.
Background And Aims: Drug discrimination procedures have made important contributions to the pre-clinical investigation of psychedelic drugs, such as psilocybin, lysergic acid diethylamide (LSD), N,N-dimethyltryptamine (DMT) and 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT). One of the most important being to highlight the critical role of central 5-HT2A receptor agonism as a mediator of hallucinogenic activity, and secondly, drugs that fully generalise to a 5-HT2A receptor agonist cued drug discrimination in rodents, may elicit hallucinogenic activity in humans, showing a forward translational value. However, there is relatively little information about how clinical exposures associated with hallucinations back-translate to generalisation profiles in the rat.
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