ArticleThe Journal of pharmacology and experimental therapeutics2010
Regional differential effects of the novel histamine H3 receptor antagonist 6-[(3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methyl-3-pyridinecarboxamide hydrochloride (GSK189254) on histamine release in the central nervous system of freely moving rats.
Article in The Journal of pharmacology and experimental therapeutics, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 65 citations in OpenAlex.
- The Diverse Network of Brain Histamine in Feeding: Dissect its Functions in a Circuit-Specific Way.Current neuropharmacology · 2024Review
- The Potent and Selective Histamine H3 Receptor Antagonist E169 Counteracts Cognitive Deficits and Mitigates Disturbances in the PI3K/AKT/GSK-3β Signaling Pathway in MK801-Induced Amnesia in Mice.International journal of molecular sciences · 2023Article
- Different Peas in the Same Pod: The Histaminergic Neuronal Heterogeneity.Current topics in behavioral neurosciences · 2022Review
- Neuronal histamine and the memory of emotionally salient events.British journal of pharmacology · 2020Review
- Histamine, histamine receptors, and neuropathic pain relief.British journal of pharmacology · 2020Review
- Histamine, histamine HBritish journal of pharmacology · 2020Review
- Histamine H3 receptor antagonist E177 attenuates amnesia induced by dizocilpine without modulation of anxiety-like behaviors in rats.Neuropsychiatric disease and treatment · 2019Article
- The Histamine H3 Receptor Antagonist DL77 Ameliorates MK801-Induced Memory Deficits in Rats.Frontiers in neuroscience · 2018Article
- Possible use of a H3R antagonist for the management of nonmotor symptoms in the Q175 mouse model of Huntington's disease.Pharmacology research & perspectives · 2017Article
- The histamine H3 receptor antagonist thioperamide rescues circadian rhythm and memory function in experimental parkinsonism.Translational psychiatry · 2017Article
- The Histamine H3 Receptor Antagonist E159 Reverses Memory Deficits Induced by Dizocilpine in Passive Avoidance and Novel Object Recognition Paradigm in Rats.Frontiers in pharmacology · 2017Article
- Interaction Between Brain Histamine and Serotonin, Norepinephrine, and Dopamine Systems: In Vivo Microdialysis and Electrophysiology Study.Journal of molecular neuroscience : MN · 2015Article
- The Effect of Subchronic Dosing of Ciproxifan and Clobenpropit on Dopamine and Histamine Levels in Rats.Journal of experimental neuroscience · 2015Article
- Differential effects of the histamine H(3) receptor agonist methimepip on dentate granule cell excitability, paired-pulse plasticity and long-term potentiation in prenatal alcohol-exposed rats.Alcoholism, clinical and experimental research · 2014Article
- Article
- Histamine H₃ receptors, the complex interaction with dopamine and its implications for addiction.British journal of pharmacology · 2013Review
- Assessment of the abuse liability of ABT-288, a novel histamine H₃ receptor antagonist.Psychopharmacology · 2013Article
- Histamine h3 receptor: a novel therapeutic target in alcohol dependence?Frontiers in systems neuroscience · 2012Article
- Histamine H3 receptor antagonists/inverse agonists on cognitive and motor processes: relevance to Alzheimer's disease, ADHD, schizophrenia, and drug abuse.Frontiers in systems neuroscience · 2012Article
- Effects of methimepip and JNJ-5207852 in Wistar rats exposed to an open-field with and without object and in Balb/c mice exposed to a radial-arm maze.Frontiers in systems neuroscience · 2012Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 2 countries.
Funding
Abstract
After oral administration, the nonimidazole histamine H(3) receptor antagonist, 6-[(3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methyl-3-pyridinecarboxamide hydrochloride (GSK189254), increased histamine release from the tuberomammillary nucleus, where all histaminergic somata are localized, and from where their axons project to the entire brain. To further understand functional histaminergic circuitry in the brain, dual-probe microdialysis was used to pharmacologically block H(3) receptors in the tuberomammillary nucleus, and monitor histamine release in projection areas. Perfusion of the tuberomammillary nucleus with GSK189254 increased histamine release from the tuberomammillary nucleus, nucleus basalis magnocellularis, and cortex, but not from the striatum or nucleus accumbens. Cortical acetylcholine (ACh) release was also increased, but striatal dopamine release was not affected. When administered locally, GSK189254 increased histamine release from the nucleus basalis magnocellularis, but not from the striatum. Thus, defined by their sensitivity to GSK189254, histaminergic neurons establish distinct pathways according to their terminal projections, and can differentially modulate neurotransmitter release in a brain region-specific manner. Consistent with its effects on cortical ACh release, systemic administration of GSK189254 antagonized the amnesic effects of scopolamine in the rat object recognition test, a cognition paradigm with important cortical components.
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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.