ArticleBritish journal of pharmacology2013
Preclinical evaluation of the abuse potential of Pitolisant, a histamine H₃ receptor inverse agonist/antagonist compared with Modafinil.
Article in British journal of pharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
23 citing papers in PubMed, 55 citations in OpenAlex.
- Trial
- Trial
- Pitolisant Inhibits Alcohol Drinking and Improves Withdrawal Negative Affect Through Lateral Habenula Histaminergic Signaling in Mice.CNS neuroscience & therapeutics · 2026Article
- Acute hypobaric hypoxia attenuates the anti-fatigue effects of pitolisant by downregulating the expression of organic cation transporter 1 and P-glycoprotein.Frontiers in pharmacology · 2025Article
- Diagnostic challenges and burden of idiopathic hypersomnia: a systematic literature review.Sleep advances : a journal of the Sleep Research Society · 2024Article
- Pitolisant: Pediatric First Approval.Paediatric drugs · 2023Review
- 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-4 Receptor: Emerging Target for the Treatment of Neurological Diseases.Current topics in behavioral neurosciences · 2022Review
- Pitolisant, a wake-promoting agent devoid of psychostimulant properties: Preclinical comparison with amphetamine, modafinil, and solriamfetol.Pharmacology research & perspectives · 2021Article
- Pitolisant: A Review in Narcolepsy with or without Cataplexy.CNS drugs · 2020Review
- Recently Approved and Upcoming Treatments for Narcolepsy.CNS drugs · 2020Review
- Pitolisant to Treat Excessive Daytime Sleepiness and Cataplexy in Adults with Narcolepsy: Rationale and Clinical Utility.Nature and science of sleep · 2020Review
- Participation of Dopamine D1 and D2 Receptors in the Rapid-Onset Behavioral Sensitization to Modafinil.Frontiers in pharmacology · 2019Article
- The histamine HNaunyn-Schmiedeberg's archives of pharmacology · 2018Article
- Profile of pitolisant in the management of narcolepsy: design, development, and place in therapy.Drug design, development and therapy · 2018Review
- Oral modafinil facilitates intracranial self-stimulation in rats: comparison with methylphenidate.Behavioural pharmacology · 2017Article
- H3 histamine receptor antagonist pitolisant reverses some subchronic disturbances induced by olanzapine in mice.Metabolic brain disease · 2016Article
- Pitolisant: First Global Approval.Drugs · 2016Review
- Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposePitolisant, a histamine H₃ receptor inverse agonist/antagonist is currently under Phase III clinical trials for treatment of excessive daytime sleepiness namely in narcoleptic patients. Its drug abuse potential was investigated using in vivo models in rodents and monkeys and compared with those of Modafinil, a psychostimulant currently used in the same indications. EXPERIMENTAL APPROACH: Effects of Pitolisant on dopamine release in the nucleus accumbens, on spontaneous and cocaine-induced locomotion, locomotor sensitization were monitored. It was also tested in three standard drug abuse tests i.e. conditioned place preference in rats, self-administration in monkeys and cocaine discrimination in mice as well as in a physical dependence model. KEY
resultsPitolisant did not elicit any significant changes in dopaminergic indices in rat nucleus accumbens whereas Modafinil increased dopamine release. In rodents, Pitolisant was without any effect on locomotion and reduced the cocaine-induced hyperlocomotion. In addition, no locomotor sensitization and no conditioned hyperlocomotion were evidenced with this compound in rats whereas significant effects were elicited by Modafinil. Finally, Pitolisant was devoid of any significant effects in the three standard drug abuse tests (including self-administration in monkeys) and in the physical dependence model. CONCLUSIONS AND IMPLICATIONS: No potential drug abuse liability for Pitolisant was evidenced in various in vivo rodent and primate models, whereas the same does not seem so clear in the case of Modafinil.
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What OpenQuestion holds
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.