ArticleBritish journal of pharmacology2012
The atypical antidepressant mianserin exhibits agonist activity at κ-opioid receptors.
Article in British journal of pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 31 citations in OpenAlex.
- Analgesic Efficacy and Tolerability of Amitriptyline versus Mianserin in Chronic Low Back Pain: A Randomised, Double-Blind, Controlled Pilot Trial.Journal of pain research · 2025Trial
- Antidepressants and the endogenous opioid system.Biochemical pharmacology · 2025Review
- α-glucan remodeling by GH13-domain enzymes shapes fungal cell wall architecture.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- Interactions of antidepressants with concomitant medications-safety of complex therapies in multimorbidities.Pharmacological reports : PR · 2024Review
- Study of Antidepressant Actions of Subanesthetic Nitrous Oxide: Importance of Adequate Blinding and Opioid Receptors.Biological psychiatry global open science · 2024Article
- DInternational journal of molecular sciences · 2024Article
- Structural insights into the unexpected agonism of tetracyclic antidepressants at serotonin receptors 5-HTScience advances · 2024Article
- Opioid Mechanisms and the Treatment of Depression.Current topics in behavioral neurosciences · 2024Review
- Structural Insights into the Unexpected Agonism of Tetracyclic Antidepressants at Serotonin Receptors 5-HT1eR and 5-HT1FR.bioRxiv : the preprint server for biology · 2023Article
- G protein-coupled receptors in neurodegenerative diseases and psychiatric disorders.Signal transduction and targeted therapy · 2023Review
- A platform utilizingProceedings of the National Academy of Sciences of the United States of America · 2021Article
- Doxepin prevents the Expression and Development of Paclitaxel-Induced Neuropathic Pain.Advanced biomedical research · 2021Article
- Psychotropic Drugs for the Management of Chronic Pain and Itch.Pharmaceuticals (Basel, Switzerland) · 2019Review
- Kappa Opioids, Salvinorin A and Major Depressive Disorder.Current neuropharmacology · 2016Review
- Metabolic bioactivation of antidepressants: advance and underlying hepatotoxicity.Drug metabolism reviewsReview
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeAntidepressants are known to interact with the opioid system through mechanisms not completely understood. We previously reported that tricyclic antidepressants act as agonists at distinct opioid receptors. Here, we investigated the effect of the atypical antidepressant mianserin at cloned and native opioid receptors. EXPERIMENTAL APPROACH: Effects of mianserin were examined in CHO cells transfected with human opioid receptors, C6 glioma cells and rat brain membranes by the use of radioligand binding and functional assays including the stimulation of [(35)S]GTPγS binding and MAPK phosphorylation. KEY
resultsMianserin displayed 12- and 18-fold higher affinity for κ- than µ- and δ-opioid receptors respectively. In [(35)S]GTPγS assays, mianserin selectively activated κ-opioid receptors. The agonist activity was antagonized by the selective κ-opioid blocker nor-binaltorphimine (nor-BNI). The mianserin analogue mirtazapine also displayed κ-opioid agonist activity. Mianserin and mirtazapine increased ERK1/2 phosphorylation in CHO cells expressing κ-opioid receptors and C6 cells, and these effects were antagonized by nor-BNI. In rat striatum and nucleus accumbens, mianserin stimulated [35S]GTPγS binding in a nor-BNI-sensitive manner with maximal effects lower than those of the full κ-opioid agonists (-)-U50,488 and dynorphin A. When combined, mianserin antagonized the effects of the full κ-opioid receptor agonists in [(35)S]GTPγS assays and reduced the stimulation of p38 MAPK and ERK1/2 phosphorylation by dynorphin A. CONCLUSIONS AND IMPLICATIONS: In different cell systems, mianserin directly activates κ-opioid receptors, displaying partial agonist activity at brain receptors. Thus, this property appears to be a common feature of different classes of antidepressants.
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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.