ArticleBritish journal of pharmacology2012
Histamine H4 receptor antagonists as potent modulators of mammalian vestibular primary neuron excitability.
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 23 papers.
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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.
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Who cites it
23 citing papers in PubMed, 52 citations in OpenAlex.
- Safety, tolerability, pharmacokinetics and pharmacokinetic-pharmacodynamic modelling of the novel HBritish journal of clinical pharmacology · 2018Trial
- Neurotransmitter regulatory networks in persistent postural-perceptual dizziness: potential mechanisms and therapeutic implications.Frontiers in neurology · 2026Review
- Targeting Histamine H4 Receptor in the Rostral Ventromedial Medulla to Relieve Hypertension.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Histaminergic System and Vestibular Function in Normal and Pathological Conditions.Current neuropharmacology · 2024Review
- Histamine and Its Receptors in the Mammalian Inner Ear: A Scoping Review.Brain sciences · 2023Article
- Chemical Probes for Histamine Receptor Subtypes.Current topics in behavioral neurosciences · 2022Article
- Histamine-4 Receptor: Emerging Target for the Treatment of Neurological Diseases.Current topics in behavioral neurosciences · 2022Review
- Effects of Several Therapeutic Agents on Mammalian Vestibular Function: Meclizine, Diazepam, and JNJ7777120.Journal of the Association for Research in Otolaryngology : JARO · 2021Article
- Effect of the novel histamine HBritish journal of pharmacology · 2020Article
- Management of peripheral vertigo with antihistamines: New options on the horizon.British journal of clinical pharmacology · 2019Review
- Histamine H4 receptor gene polymorphisms: a potential contributor to Meniere disease.BMC medical genomics · 2019Article
- To scratch an itch: Establishing a mouse model to determine active brain areas involved in acute histaminergic itch.IBRO reports · 2018Article
- Effect of M-current modulation on mammalian vestibular responses to transient head motion.Journal of neurophysiology · 2017Article
- Neuropharmacological Targets for Drug Action in Vestibular Sensory Pathways.Journal of audiology & otology · 2017Review
- Article
- Correlation between afferent rearrangements and behavioral deficits after local excitotoxic insult in the mammalian vestibule: a rat model of vertigo symptoms.Disease models & mechanisms · 2016Article
- Evidence for a Role of Orexin/Hypocretin System in Vestibular Lesion-Induced Locomotor Abnormalities in Rats.Frontiers in neuroscience · 2016Article
- Motion Sickness: Current Knowledge and Recent Advance.CNS neuroscience & therapeutics · 2016Review
- Transient alteration of the vestibular calyceal junction and synapse in response to chronic ototoxic insult in rats.Disease models & mechanisms · 2015Article
- International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.Pharmacological reviews · 2015Review
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeBetahistine, the main histamine drug prescribed to treat vestibular disorders, is a histamine H(3) receptor antagonist. Here, we explored the potential for modulation of the most recently cloned histamine receptor (H(4) receptor) to influence vestibular system function, using a selective H(4) receptor antagonist JNJ 7777120 and the derivate compound JNJ 10191584. EXPERIMENTAL APPROACH: RT-PCR was used to assess the presence of H(4) receptors in rat primary vestibular neurons. In vitro electrophysiological recordings and in vivo behavioural approaches using specific antagonists were employed to examine the effect of H(4) receptor modulation in the rat vestibular system. KEY
resultsThe transcripts of H(4) and H(3) receptors were present in rat vestibular ganglia. Application of betahistine inhibited the evoked action potential firing starting at micromolar range, accompanied by subsequent strong neuronal depolarization at higher concentrations. Conversely, reversible inhibitory effects elicited by JNJ 10191584 and JNJ 7777120 began in the nanomolar range, without inducing neuronal depolarization. This effect was reversed by application of the selective H(4) receptor agonist 4-methylhistamine. Thioperamide, a H(3) /H(4) receptor antagonist, exerted effects similar to those of H(3) and H(4) receptor antagonists, namely inhibition of firing at nanomolar range and membrane depolarization above 100 µM. H(4) receptor antagonists significantly alleviated the vestibular deficits induced in rats, while neither betahistine nor thioperamide had significant effects. CONCLUSIONS AND IMPLICATIONS: H(4) receptor antagonists have a pronounced inhibitory effect on vestibular neuron activity. This result highlights the potential role of H(4) receptors as pharmacological targets for the treatment of vestibular disorders.
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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.