ArticleACS chemical neuroscience2013
Synergism between a serotonin 5-HT2A receptor (5-HT2AR) antagonist and 5-HT2CR agonist suggests new pharmacotherapeutics for cocaine addiction.
Article in ACS chemical neuroscience, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 58 papers.
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Who cites it
58 citing papers in PubMed.
- Trial
- Citalopram for treatment of cocaine use disorder: A Bayesian drop-the-loser randomized clinical trial.Drug and alcohol dependence · 2021Trial
- The psychedelic (-)-2,5-dimethoxy-4-iodoamphetamine [(-)-DOI] demonstrates efficacy in reducing cocaine reward and motivation in male rats.Psychopharmacology · 2025Article
- Withdrawal from chronic alcohol impairs the serotonin-mediated modulation of GABAergic transmission in the infralimbic cortex in male rats.Neurobiology of disease · 2024Article
- Novel therapeutics in development for the treatment of stimulant-use disorder.Current opinion in neurobiology · 2024Review
- Nelotanserin, a selective 5-HT2A receptor inverse agonist, attenuates aspects of nicotine withdrawal but not reward in mice.Behavioural brain research · 2024Article
- Social stress-induced serotonin dysfunction activates spexin in male Nile tilapia (Proceedings of the National Academy of Sciences of the United States of America · 2023Article
- Ghrelin receptor antagonist JMV2959 blunts cocaine and oxycodone drug-seeking, but not self-administration, in male rats.Frontiers in pharmacology · 2023Article
- μ-opioid receptor agonists and psychedelics: pharmacological opportunities and challenges.Frontiers in pharmacology · 2023Review
- Role of 5-HTPsychopharmacology · 2022Article
- A serotonergic biobehavioral signature differentiates cocaine use disorder participants administered mirtazapine.Translational psychiatry · 2022Article
- Interactions between impulsivity and MDPV self-administration in rats.Addiction biology · 2022Article
- Machine Learning Analysis of Cocaine Addiction Informed by DAT, SERT, and NET-Based Interactome Networks.Journal of chemical theory and computation · 2022Article
- Heightened cocaine-seeking in male rats associates with a distinct transcriptomic profile in the medial prefrontal cortex.Frontiers in pharmacology · 2022Article
- Class A and C GPCR Dimers in Neurodegenerative Diseases.Current neuropharmacology · 2022Review
- International Union of Basic and Clinical Pharmacology. CX. Classification of Receptors for 5-hydroxytryptamine; Pharmacology and Function.Pharmacological reviews · 2021Review
- Blockade of 5-Hydroxytryptamine 2A Receptor Attenuates Precipitation of Naloxone-Induced Withdrawal Symptoms in Opioid-Exposed Mice.Frontiers in behavioral neuroscience · 2021Article
- Discovery of Potent and Brain-Penetrant GPR52 Agonist that Suppresses Psychostimulant Behavior.Journal of medicinal chemistry · 2020Article
- Cocaine reward and memory after chemogenetic inhibition of distinct serotonin neuron subtypes in mice.Psychopharmacology · 2020Article
- Suppression of cocaine relapse-like behaviors upon pimavanserin and lorcaserin co-administration.Neuropharmacology · 2020Article
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Authors and funding
11 authors.
Funding
Abstract
Relapse to cocaine dependence, even after extended abstinence, involves a number of liability factors including impulsivity (predisposition toward rapid, unplanned reactions to stimuli without regard to negative consequences) and cue reactivity (sensitivity to cues associated with cocaine-taking which can promote cocaine-seeking). These factors have been mechanistically linked to serotonin (5-hydroxytryptamine, 5-HT) signaling through the 5-HT(2A) receptor (5-HT(2A)R) and 5-HT(2C)R; either a selective 5-HT(2A)R antagonist or a 5-HT(2C)R agonist suppresses impulsivity and cocaine-seeking in preclinical models. We conducted proof-of-concept analyses to evaluate whether a combination of 5-HT(2A)R antagonist plus 5-HT(2C)R agonist would have synergistic effects over these liability factors for relapse as measured in a 1-choice serial reaction time task and cocaine self-administration/reinstatement assay. Combined administration of a dose of the selective 5-HT(2A)R antagonist M100907 plus the 5-HT(2C)R agonist WAY163909, each ineffective alone, synergistically suppressed cocaine-induced hyperactivity, inherent and cocaine-evoked impulsive action, as well as cue- and cocaine-primed reinstatement of cocaine-seeking behavior. The identification of synergism between a 5-HT(2A)R antagonist plus a 5-HT(2C)R agonist to attenuate these factors important in relapse indicates the promise of a bifunctional ligand as an anti-addiction pharmacotherapeutic, setting the stage to develop new ligands with improved efficacy, potency, selectivity, and in vivo profiles over the individual molecules.
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