SAR110894, a potent histamine H3-receptor antagonist, displays procognitive effects in rodents

Griebel, Guy; Pichat, Philippe; Pruniaux, Marie-Pierre; Beeské, Sandra; Lopez-Grancha, Mati; Genet, Elisabeth; Terranova, Jean-Paul; Castro, Antonio de; Sánchez, Juan Antonio; Black, Mark D.; Varty, Geoffrey B.; Weiner, Ina; Arad, Michal; Barak, Segev; Levie, Amaya De; Guillot, Etienne

doi:10.1016/j.pbb.2012.04.004

Cited by 40 publications

(33 citation statements)

References 44 publications

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“…12 are in line with previous reports that various H 3 R antagonists (thioperamide and clobenpropit (Giovannini et al, 1999); pitolisant (Ligneau et al, 2007); GSK189254 (Giannoni et al, 2010); SAR110894 (Griebel et al, 2012) antagonize the amnesic effects of scopolamine, MK801 or time in the rat and mouse ORT.…”

Section: A C C E P T E D Accepted Manuscriptsupporting

confidence: 90%

Donepezil, an acetylcholine esterase inhibitor, and ABT-239, a histamine H3 receptor antagonist/inverse agonist, require the integrity of brain histamine system to exert biochemical and procognitive effects in the mouse

et al. 2016

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Section: A C C E P T E D Accepted Manuscriptsupporting

confidence: 90%

Donepezil, an acetylcholine esterase inhibitor, and ABT-239, a histamine H3 receptor antagonist/inverse agonist, require the integrity of brain histamine system to exert biochemical and procognitive effects in the mouse

et al. 2016

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“…failed to alter time spent in the center arena, time spent in the periphery, total time spent for locomotion, total distance traveled, occurrence of rearing, and incidence of grooming. The data are expressed as the mean ± SEM (n=6-7 observations in earlier preclinical studies in which various imidazole-based H3R antagonists, such as thioperamide and clobenpropit, 65 and non-imidazole-based H3R antagonists, such as pitolisant, GSK189254, SAR110894, ABT-239, and E159, 53,[66][67][68][69] attenuated the memory impairment induced by DIZ and scopolamine in the NOR task in a variety of animal species. In the current study, the H3R antagonist E177 appreciably counteracted the STM impairment associated with DIZ treatment, and the observed protective effect of E177 was completely reversed when the H3R agonist RAMH was co-injected ( Figure 4A; Table 1).…”

Section: Discussionmentioning

confidence: 99%

<p>Histamine H3 receptor antagonist E177 attenuates amnesia induced by dizocilpine without modulation of anxiety-like behaviors in rats</p>

Alachkar¹,

Khan²,

Łażewska³

et al. 2019

NDT

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Background: Alzheimer disease (AD) is the main cause of dementia in elderly people. The potential of histamine H3 receptor (H3R) antagonists as a pharmacological treatment of several neuropsychiatric diseases is well established. Methods: The novel non-imidazole-based H3R antagonist E177 was screened for its procognitive effects on the inhibitory avoidance paradigm (IAP) and novel object recognition (NOR) task in a dizocilpine (DIZ)-induced model of amnesia in male Wistar rats. Donepezil, an acetylcholine esterase inhibitor, was used as the reference drug. Results: Acute systemic treatment with E177 (1.25, 2.5, 5, and 10 mg/kg intraperitoneally [i.p.]) significantly attenuated the cognitive impairments induced by DIZ in the IAP (all P-values ,0.05, n=7), and the protective effect of the most promising dose of E177 (5 mg/kg) was abrogated when H3R agonist R-(α)-methylhistamine (RAMH; 10 mg/kg i.p.) was co-administered (P=0.281 for DIZ-amnesia group vs DIZ + E177 + RAMH group, n=7). The discrimination index calculated for E177 (5 mg/kg, i.p.) showed a significant memory-enhancing effect on DIZ-induced shortterm memory impairment in the NOR task (P,0.05, n=6), with the enhancement nullified when animals were co-administered RAMH (10 mg/kg). Moreover, the results revealed that E177 (5 and 10 mg/kg, i.p.) did not alter the anxiety levels and locomotor activity of animals naïve to the open-field test (all P-values .0.05, n=8) or the elevated plus maze test (all P-values .0.05, n=6-8), which indicated that the E177-induced enhancement of memory performance in the IAP or NOR task was unrelated to changes in emotional response or in spontaneous locomotor activity. Conclusion: The observed results suggested a possible contribution of H3Rs in the alteration of brain neurotransmitters that accompany neurodegenerative diseases, such as AD.

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“…(Figure 10, Table 1&4). Also, the highly potent and selective H3R antagonist SAR-110894 reversed a deficit in working memory in the Y-maze test in rodents (Figure 10, Table 1) [110]. Based on these findings, SAR-110894 has been suggested to be of therapeutic interest for the treatment of the cognitive symptoms of AD, and it has completed a phase 2 clinical study for mild-moderate AD in which it was tested as an additive to the standard drug donepezil with no disclosure of the results for both clinical trials (Figure 10, Table 1).…”

Section: Alzheimer's Diseasementioning

confidence: 95%

Histamine H3 receptor as a potential target for cognitive symptoms in neuropsychiatric diseases

Sadek

Saad

Sadeq

et al. 2016

Behavioural Brain Research

125

123

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SAR110894, a potent histamine H3-receptor antagonist, displays procognitive effects in rodents

Cited by 40 publications

References 44 publications

Donepezil, an acetylcholine esterase inhibitor, and ABT-239, a histamine H3 receptor antagonist/inverse agonist, require the integrity of brain histamine system to exert biochemical and procognitive effects in the mouse

Donepezil, an acetylcholine esterase inhibitor, and ABT-239, a histamine H3 receptor antagonist/inverse agonist, require the integrity of brain histamine system to exert biochemical and procognitive effects in the mouse

<p>Histamine H3 receptor antagonist E177 attenuates amnesia induced by dizocilpine without modulation of anxiety-like behaviors in rats</p>

Histamine H3 receptor as a potential target for cognitive symptoms in neuropsychiatric diseases

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