ArticleCurrent pharmaceutical design2015
Atypical antipsychotics and inverse agonism at 5-HT2 receptors.
Article in Current pharmaceutical design, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
21 citing papers in PubMed.
- Are Depot Antipsychotics Ever Self-Tapering? Exploring the Discontinuation of Long-Acting Injectable Psychosis Drugs and Those With Delayed Onset Through In Silico Modelling.Schizophrenia bulletin open · 2026Article
- The Effect of Semaglutide With Lifestyle Intervention on the Physical Health of Patients Treated With Antipsychotic Drugs in a Secure Mental Health Setting: Protocol for an Uncontrolled Pretest-Posttest Pilot Mixed Methods Study.JMIR research protocols · 2025Article
- Distinctive patterns of G protein coupling induced by the structurally similar 5-HTMolecular pharmacology · 2025Article
- Pharmacological fingerprint of antipsychotic drugs at the serotonin 5-HTMolecular psychiatry · 2024Article
- Examining the Use of Oral Aripiprazole in Patients With Autism Spectrum Disorder: A Study of Retrospective Chart Review at a University Medical Center.Journal of the Korean Academy of Child and Adolescent Psychiatry · 2024Article
- DRD2, DRD3, and HTR2A Single-Nucleotide Polymorphisms Involvement in High Treatment Resistance to Atypical Antipsychotic Drugs.Biomedicines · 2023Article
- Cerebral chemoarchitecture shares organizational traits with brain structure and function.eLife · 2023Article
- Aripiprazole Offsets Mutant ATXN3-Induced Motor Dysfunction by Targeting Dopamine DBiomedicines · 2022Article
- Experimental Serotonergic Agents for the Treatment of Schizophrenia.Journal of experimental pharmacology · 2021Review
- International Union of Basic and Clinical Pharmacology. CX. Classification of Receptors for 5-hydroxytryptamine; Pharmacology and Function.Pharmacological reviews · 2021Review
- A Novel Synthetic Interfering Peptide Tat-3L4F Attenuates Olanzapine-Induced Weight Gain Through Disrupting Crosstalk Between Serotonin Receptor 2C and Protein Phosphatase and Tensin Homolog in Rats.The international journal of neuropsychopharmacology · 2020Article
- Current and Novel Approaches to Mitigate Cardiometabolic Adverse Effects of Second-Generation Antipsychotics.The international journal of neuropsychopharmacology · 2020Article
- Neurochemical Evidence of Preclinical and Clinical Reports on Target-Based Therapy in Alcohol Used Disorder.Neurochemical research · 2020Review
- Exploring mechanisms of increased cardiovascular disease risk with antipsychotic medications: Risperidone alters the cardiac proteomic signature in mice.Pharmacological research · 2020Article
- Human biodistribution and radiation dosimetry of the 5-HTEJNMMI research · 2019Article
- Signaling characteristics and functional regulation of delta opioid-kappa opioid receptor (DOP-KOP) heteromers in peripheral sensory neurons.Neuropharmacology · 2019Article
- Role of mGlu2 in the 5-HTPsychopharmacology · 2018Article
- Making Sense of Pharmacology: Inverse Agonism and Functional Selectivity.The international journal of neuropsychopharmacology · 2018Review
- A short history of the 5-HTPsychopharmacology · 2017Review
- Pimavanserin: A novel therapeutic option for Parkinson disease psychosis.Neurology. Clinical practice · 2017Review
Corrections and comments
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Authors and funding
3 authors.
Funding
Abstract
It is now well accepted that receptors can regulate cellular signaling pathways in the absence of a stimulating ligand, and inverse agonists can reduce this ligand-independent or "constitutive" receptor activity. Both the serotonin 5-HT2A and 5-HT2C receptors have demonstrated constitutive receptor activity in vitro and in vivo. Each has been identified as a target for treatment of schizophrenia. Further, most, if not all, atypical antipsychotic drugs have inverse agonist properties at both 5-HT2A and 5-HT2C receptors. This paper describes our current knowledge of inverse agonism of atypical antipsychotics at 5-HT2A/2C receptor subtypes in vitro and in vivo. Exploiting inverse agonist properties of APDs may provide new avenues for drug development.
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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.