Serotonin receptor affinity and photelectron spectral data were obtained on a number of substituted N,N-dimethyltryptamines. Evidence is presented that electron-donating substituents in the 5-position lead to enhanced behavioral disruption activity and serotonin receptor affinity as compared to unsubstituted N,N-dimethyltryptamine and analogues substituted in the 4- or 6-position. Some correlation was found between ionization potentials and behavioral activity, which may have implications concerning the mechanism of receptor binding.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/jm00353a021 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Randomized Controlled Trial of the Effects of High-Dose Ondansetron on Clinical Symptoms and Brain Connectivity in Obsessive-Compulsive and Tic Disorders.
Am J Psychiatry
January 2025
Nathan Kline Institute for Psychiatric Research, Orangeburg, NY (Stern, Collins, Bragdon, Eng, Recchia, Tobe, Iosifescu); Department of Psychiatry (Stern, Bragdon, Eng, Recchia, Iosifescu) and Neuroscience Institute (Stern, Iosifescu), New York University Langone Medical Center, New York; Department of Psychiatry, University of Miami Medical School, Miami (Coffey); Department of Psychiatry, Icahn School of Medicine at Mount Sinai, New York (Leibu, Murrough); Center for the Developing Brain, Child Mind Institute, New York (Tobe); Department of Psychiatry, Brigham and Women's Hospital, Boston (Burdick); Harvard Medical School, Boston (Burdick); Department of Psychiatry, Baylor College of Medicine, Houston (Goodman).
Objective: Sensory phenomena (SP) are aversive sensations driving repetitive behaviors in obsessive-compulsive disorder (OCD) and Tourette's disorder that are not well addressed by standard treatments. SP are related to the functioning of an interoceptive-sensorimotor circuit that may be modulated by the 5-HT receptor antagonist ondansetron. The present study employed an experimental medicine approach to test the effects of 4 weeks of high-dose ondansetron compared to placebo on SP severity and brain connectivity in a cohort of individuals with OCD and/or Tourette's disorder.
View Article and Find Full Text PDFThyroid Endocrine Disrupting Potential of Fluoxetine in Zebrafish Larvae.
J Appl Toxicol
January 2025
Changjiang Basin Ecology and Environment Monitoring and Scientific Research Center, Changjiang Basin Ecology and Environment Administration, Ministry of Ecology and Environment, Wuhan, China.
Fluoxetine (FLX), a typical selective serotonin reuptake inhibitors, has been frequently detected in aquatic environment and wild fish. However, little is known about its effect on thyroid endocrine system. In the present study, zebrafish (Danio rerio) embryos were exposed to 1, 3, 10, and 30 μg/L of FLX for 6 days.
View Article and Find Full Text PDFThe role of rodent behavioral models of schizophrenia in the ongoing search for novel antipsychotics.
Expert Opin Drug Discov
January 2025
Centro de Investigación en Reproducción Animal, Universidad Autónoma de Tlaxcala - CINVESTAV Tlaxcala, Tlaxcala, México.
Introduction: Existing pharmacotherapies for schizophrenia have not progressed beyond targeting dopamine and serotonin neurotransmission. Rodent models of schizophrenia are a necessary tool for elucidating neuropathological processes and testing potential pharmacotherapies, but positive preclinical results in rodent models often do not translate to positive results in the clinic.
Areas Covered: The authors reviewed PubMed for studies that applied rodent behavioral models of schizophrenia to assess the antipsychotic potential of several novel pharmacotherapies currently under investigation.
Trace amine signaling in zebrafish models: CNS pharmacology, behavioral regulation and translational relevance.
Eur J Pharmacol
January 2025
Institute of Translational Biomedicine (ITBM), St. Petersburg State University, St. Petersburg, Russia; Department of Biosciences and Bioinformatics, School of Science, Xi'an Jiaotong-Liverpool University, Suzhou, China; Suzhou Municipal Key Laboratory of Neurobiology and Cell Signaling, School of Science, Xi'an Jiaotong-Liverpool University, Suzhou, China. Electronic address:
Tyramine, β-phenylethylamine, octopamine and other trace amines are endogenous substances recently recognized as important novel neurotransmitters in the brain. Trace amines act via multiple selective trace amine-associated receptors (TAARs) of the G protein-coupled receptor family. TAARs are expressed in various brain regions and modulate neurotransmission, neuronal excitability, adult neurogenesis, cognition, mood, locomotor activity and olfaction.
View Article and Find Full Text PDFToxicodynamic insights of 2C and NBOMe drugs - Is there abuse potential?
Toxicol Rep
June 2025
Associate Laboratory i4HB-Institute for Health and Bioeconomy, Faculty of Pharmacy, University of Porto, Porto, Portugal.
Drug use represents a prevalent and multifaceted societal problem, with profound implications for public health, social welfare, and economic stability. To circumvent strict international drug control regulations, there is a growing trend in the development and market introduction of novel psychoactive substances (NPS), encompassing a wide range of compounds with psychoactive properties. This includes, among other classes of drugs, the phenethylamines.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!