ArticleNeuroscience2011
Psychotropic and nonpsychotropic cannabis derivatives inhibit human 5-HT(3A) receptors through a receptor desensitization-dependent mechanism.
Article in Neuroscience, 2011. 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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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.
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Who cites it
15 citing papers in PubMed, 31 citations in OpenAlex.
- The Pharmacological Profile of Plant-Derived Cannabinoids In Vitro.Current topics in behavioral neurosciences · 2026Review
- Predicting Δ-9-Tetrahydrocannabinol-Induced Psychoactive and Cognitive Effects: A PBPK-PD Approach to Quantifying Feeling High and Reduced Alertness.ACS chemical neuroscience · 2025Article
- Beyond the hype: a comprehensive exploration of CBD's biological impacts and mechanisms of action.Journal of cannabis research · 2025Review
- Medicinal Plants for Chemotherapy-Induced Nausea and Vomiting: A Systematic Review of Antiemetic, Chemosensitizing, and Immunomodulatory Mechanisms.Therapeutics and clinical risk management · 2025Review
- A review of the direct targets of the cannabinoids cannabidiol, Δ9-tetrahydrocannabinol, N-arachidonoylethanolamine and 2-arachidonoylglycerol.AIMS neuroscience · 2024Review
- The Polypharmacological Effects of Cannabidiol.Molecules (Basel, Switzerland) · 2023Review
- Cannabidiol as a modulator of α7 nicotinic receptors.Cellular and molecular life sciences : CMLS · 2022Article
- Effects of cannabinoids on ligand-gated ion channels.Frontiers in physiology · 2022Review
- Computational Approach Reveals Pronociceptive Potential of Cannabidiol in Osteoarthritis: Role of Transient Receptor Potential Channels.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Neuromolecular Mechanisms of Cannabis Action.Advances in experimental medicine and biology · 2021Review
- Membrane cholesterol dependence of cannabinoid modulation of glycine receptor.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2020Article
- Cannabidiol Affects the Bezold-Jarisch ReflexFrontiers in pharmacology · 2019Article
- Multiple mechanisms involved in the large-spectrum therapeutic potential of cannabidiol in psychiatric disorders.Philosophical transactions of the Royal Society of London. Series B, Biological sciences · 2012Review
- The anti-nausea effects of CB1 agonists are mediated by an action at the visceral insular cortex.British journal of pharmacology · 2012Article
- Psychotropic and nonpsychotropic cannabis derivatives inhibit human 5-HT(3A) receptors through a receptor desensitization-dependent mechanism.Neuroscience · 2011Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
Abstract
Δ⁹ tetrahydrocannabinol (THC) and cannabidiol (CBD) are the principal psychoactive and nonpsychoactive components of cannabis. While most THC-induced behavioral effects are thought to depend on endogenous cannabinoid 1 (CB1) receptors, the molecular targets for CBD remain unclear. Here, we report that CBD and THC inhibited the function of human 5-HT(3A) receptors (h5-HT(3A)Rs) expressed in HEK 293 cells. The magnitude of THC and CBD inhibition was maximal 5 min after a continuous incubation with cannabinoids. The EC₅₀ values for CBD and THC-induced inhibition were 110 nM and 322 nM, respectively in HEK 293 cells expressing h5-HT(3A)Rs. In these cells, CBD and THC did not stimulate specific [³⁵S]-GTP-γs binding in membranes, suggesting that the inhibition by cannabinoids is unlikely mediated by a G-protein dependent mechanism. On the other hand, both CBD and THC accelerated receptor desensitization kinetics without significantly changing activation time. The extent of cannabinoid inhibition appeared to depend on receptor desensitization. Reducing receptor desensitization by nocodazole, 5-hydroxyindole and a point-mutation in the large cytoplasmic domain of the receptor significantly decreased CBD-induced inhibition. Similarly, the magnitude of THC and CBD-induced inhibition varied with the apparent desensitization rate of h5-HT(3A)Rs expressed in Xenopus oocytes. For instance, with increasing amount of h5-HT(3A)R cRNA injected into the oocytes, the receptor desensitization rate at steady state decreased. THC and CBD-induced inhibition was correlated with the change in the receptor desensitization rate. Thus, CBD and THC inhibit h5-HT(3A) receptors through a mechanism that is dependent on receptor desensitization.
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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.