ArticleThe pharmacogenomics journal
Pharmacologic analysis of non-synonymous coding h5-HT2A SNPs reveals alterations in atypical antipsychotic and agonist efficacies.
Article in The pharmacogenomics journal. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 52 citations in OpenAlex.
- Genome-wide pharmacogenomic analysis of response to treatment with antipsychotics.Molecular psychiatry · 2011Trial
- Psychedelics: preclinical insights provide directions for future research.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2024Review
- Mechanisms and molecular targets surrounding the potential therapeutic effects of psychedelics.Molecular psychiatry · 2023Review
- The promises and perils of psychedelic pharmacology for psychiatry.Nature reviews. Drug discovery · 2022Review
- Understanding the Effects of Antipsychotics on Appetite Control.Frontiers in nutrition · 2021Review
- Indolethylamine-Frontiers in neuroscience · 2018Review
- Family-based clinical associations and functional characterization of the serotonin 2A receptor gene (HTR2A) in autism spectrum disorder.Autism research : official journal of the International Society for Autism Research · 2014Article
- Serotonin 2A receptor gene (HTR2A) regulatory variants: possible association with severity of depression symptoms in children with autism spectrum disorder.Cognitive and behavioral neurology : official journal of the Society for Behavioral and Cognitive Neurology · 2014Article
- Pharmacogenomics can improve antipsychotic treatment in schizophrenia.Frontiers of medicine · 2013Review
- Multiple regulatory variants modulate expression of 5-hydroxytryptamine 2A receptors in human cortex.Biological psychiatry · 2013Article
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
The 5-HT(2A)-serotonin receptor is a major molecular target for most atypical antipsychotic drugs as well as most hallucinogens, which can exacerbate psychotic symptoms. In this study, we examined whether random sequence variations in the gene (single nucleotide polymorphisms, SNPs) encoding the 5-HT(2A)-serotonin receptor could explain inter-individual variability in atypical antipsychotic and agonist drug response. We examined the in vitro pharmacology of four non-synonymous SNPs, which give rise to T25N, I197V, A447V, and H452Y variant 5-HT(2A)-serotonin receptors. Our data indicate that these non-synonymous SNPs exert statistically significant, although modest, effects on the affinity and functional effects of several currently approved atypical antipsychotics (aripiprazole, clozapine, olanzapine, quetiapine, risperidone, and ziprasidone). Also, the 5-HT(2A) receptor SNPs slightly altered the potency and relative efficacy of a small number of selected agonists (2,5-dimethoxy-4-iodoamphetamine, tryptamine, 5-hydroxytryptamine, m-chlorophenylpiperazine, and 5-methoxy-N, N-dimethyltryptamine). In all, our results show that the in vitro pharmacological effects of the SNPs are drug specific.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.