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Pitolisant

Catalog No. T60636 CAS 362665-56-3

Pitolisant is a potent and selective nonimidazole inverse agonist that acts on the recombinant human histamine H3 receptor with Ki of 0.16 nM.

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Pitolisant, CAS 362665-56-3

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Description	Pitolisant is a potent and selective nonimidazole inverse agonist that acts on the recombinant human histamine H3 receptor with Ki of 0.16 nM.
In vitro	Upon stimulating guanosine 5′-O-(3-[35S]thio)triphosphate binding to its receptor, Pitolisant (BF2.649) serves as a competitive antagonist with a K_i value of 0.16 nM, and as an inverse agonist with an EC_50 of 1.5 nM, showing an intrinsic activity approximately 50% greater than ciproxifan. It also dislodges [125I]iodoproxyfan from mouse brain cortical membranes, exhibiting an IC_50 of 26.4±4.5 nM; given the radioligand's K_d of 161±9 pM, the estimated K_i for Pitolisant is 14±1 nM. Furthermore, Pitolisant interrupts [125I]iodoproxyfan interaction with membranes from rat glioma C6 cells expressing the human H3 receptor, demonstrated by an IC_50 of 4.2±0.2 nM; with the radioligand's K_d being 50±4 pM, the inferred K_i sits at 2.7±0.5 nM. It also systematically reverses this interaction with a Hill coefficient nearing one and an IC_50 of 330±68 nM, resulting in a calculated K_i of 17±4 nM. Lastly, Pitolisant induces a dose-related reduction in the basal-specific [35S]GTPγS attachment to membranes, attaining a maximum effect of 75±1% of the basal-specific binding, paired with an EC_50 of 1.5±0.1 nM.
In vivo	Administering a single 10 mg/kg dose of Pitolisant 30 minutes before a single dose of Olanzapine (2 mg/kg b.w.) significantly impacts immobility time in the Forced Swim Test (FST), markedly increasing immobility duration in mice compared to the control group. This treatment sequence also reduces locomotor activity. However, subchronic administration of these drugs (Pitolisant 10 mg/kg b.w., followed by Olanzapine 2 mg/kg b.w. 30 minutes later, and a second dose of Olanzapine 2 mg/kg b.w. after 4 hours) over fifteen sessions normalizes locomotor activity to levels observed in the control group, which received only Pitolisant. Crucially, this regimen substantially diminishes immobility times in the FST to those seen in the control group, as demonstrated by statistical analysis [one-way ANOVA; F (3,20) =4.226, P=0.0181] [2]. Additionally, rats administered Pitolisant (10 mg/kg) during the conditioning phase did not exhibit a statistically significant difference in time spent on the paired texture compared to controls, indicating no development of place preference with Pitolisant [3].

Molecular Weight	295.85
Formula	C17H26ClNO
CAS No.	362665-56-3

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

Pitolisant 362665-56-3 inhibitor inhibit

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