ArticleBritish journal of pharmacology2004
Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist.
Article in British journal of pharmacology, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 35 papers.
What it found
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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.
The trial behind it
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Who cites it
35 citing papers in PubMed, 142 citations in OpenAlex.
- Binding affinities for histamine receptors 1 to 4: Systematic comparison of ligands from the Psychoactive Drug Screening Program KMolecular pharmacology · 2026Review
- Insomnia-related rodent models in drug discovery.Acta pharmacologica Sinica · 2024Review
- Histaminergic regulation of food intake.Frontiers in endocrinology · 2023Review
- The Novel Pimavanserin Derivative ST-2300 with Histamine HBiomolecules · 2022Article
- Chemical Probes for Histamine Receptor Subtypes.Current topics in behavioral neurosciences · 2022Article
- Therapeutic Potential of Histamine H3 Receptors in Substance Use Disorders.Current topics in behavioral neurosciences · 2022Review
- Histamine HBiological psychiatry · 2021Article
- The histamine HNaunyn-Schmiedeberg's archives of pharmacology · 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
- International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.Pharmacological reviews · 2015Review
- Role of histamine H3 receptor in glucagon-secreting αTC1.6 cells.FEBS open bio · 2015Article
- Procognitive properties of drugs with single and multitargeting H3 receptor antagonist activities.CNS neuroscience & therapeutics · 2014Review
- The expression and function of histamine H₃ receptors in pancreatic beta cells.British journal of pharmacology · 2014Article
- The dual H3/4R antagonist thioperamide does not fully mimic the effects of the 'standard' H4R antagonist JNJ 7777120 in experimental murine asthma.Naunyn-Schmiedeberg's archives of pharmacology · 2013Article
- Review
- Modafinil as a catecholaminergic agent: empirical evidence and unanswered questions.Frontiers in neurology · 2013Review
- Assessment of the abuse liability of ABT-288, a novel histamine H₃ receptor antagonist.Psychopharmacology · 2013Article
- Preclinical evaluation of the abuse potential of Pitolisant, a histamine H₃ receptor inverse agonist/antagonist compared with Modafinil.British journal of pharmacology · 2013Article
- Enhanced histaminergic neurotransmission and sleep-wake alterations, a study in histamine H3-receptor knock-out mice.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2013Article
- Natriuretic peptide-induced catecholamine release from cardiac sympathetic neurons: inhibition by histamine H3 and H4 receptor activation.The Journal of pharmacology and experimental therapeutics · 2012Article
Corrections and comments
- Erratum issued
Authors and funding
15 authors at 1 institution in 1 country.
Funding
Abstract
1 1-[4-(3-piperidin-1-yl-propoxy)-benzyl]-piperidine (JNJ-5207852) is a novel, non-imidazole histamine H3 receptor antagonist, with high affinity at the rat (pKi=8.9) and human (pKi=9.24) H3 receptor. JNJ-5207852 is selective for the H3 receptor, with negligible binding to other receptors, transporters and ion channels at 1 microm. 2 JNJ-5207852 readily penetrates the brain tissue after subcutaneous (s.c.) administration, as determined by ex vivo autoradiography (ED50 of 0.13 mg kg(-1) in mice). In vitro autoradiography with 3H-JNJ-5207852 in mouse brain slices shows a binding pattern identical to that of 3H-R-alpha-methylhistamine, with high specific binding in the cortex, striatum and hypothalamus. No specific binding of 3H-JNJ-5207852 was observed in brains of H3 receptor knockout mice. 3 In mice and rats, JNJ-5207852 (1-10 mg kg(-1) s.c.) increases time spent awake and decreases REM sleep and slow-wave sleep, but fails to have an effect on wakefulness or sleep in H3 receptor knockout mice. No rebound hypersomnolence, as measured by slow-wave delta power, is observed. The wake-promoting effects of this H3 receptor antagonist are not associated with hypermotility. 4 A 4-week daily treatment of mice with JNJ-5207852 (10 mg kg(-1) i.p.) did not lead to a change in body weight, possibly due to the compound being a neutral antagonist at the H3 receptor. 5 JNJ-5207852 is extensively absorbed after oral administration and reaches high brain levels. 6 The data indicate that JNJ-5207852 is a novel, potent and selective H3 antagonist with good in vitro and in vivo efficacy, and confirm the wake-promoting effects of H3 receptor antagonists.
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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.