Pitolisant hydrochloride

Catalog No.S5926 Synonyms: Tiprolisant hydrochloride, BF-2649 HCl

For research use only.

Pitolisant (Tiprolisant, BF-2649) acts as a high-affinity competitive antagonist (Ki=0.16 nM) and as an inverse agonist (EC50=1.5 nM) at the human histamine H3 receptor subtype.

Pitolisant hydrochloride Chemical Structure

CAS No. 903576-44-3

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Biological Activity

Description Pitolisant (Tiprolisant, BF-2649) acts as a high-affinity competitive antagonist (Ki=0.16 nM) and as an inverse agonist (EC50=1.5 nM) at the human histamine H3 receptor subtype.
Targets
H3 receptor [1]
0.16 nM(Ki)
In vitro

Pitolisant shows high selectivity for H3 receptors compared with the other histamine receptor subtypes (H1, H2, and H4 subtypes) and shows a lack of interaction with other human receptors or channels[1].

In vivo In animal experiments, pitolisant increases histaminergic and noradrenergic neuron activity, increases wakefulness at the expense of slow wave and rapid eye movement sleep, has low abuse potential, and has no effect on mechanical or thermal pain thresholds[1].

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 332.31
Formula

C17H27Cl2NO

CAS No. 903576-44-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CCN(CC1)CCCOCCCC2=CC=C(C=C2)Cl.Cl

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05458128 Not yet recruiting Drug: pitolisant Idiopathic Hypersomnia|Excessive Daytime Sleepiness Harmony Biosciences LLC August 2022 Phase 3
NCT02929342 Completed Drug: Pitolisant|Radiation: [14C]-Pitolisant Healthy Volunteers Bioprojet July 2016 Phase 1
NCT02611687 Active not recruiting Drug: pitolisant|Drug: Placebo Narcolepsy With Cataplexy|Narcolepsy Without Cataplexy Bioprojet June 6 2016 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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