Home Neuronal Signaling Histamine Receptor antagonist Pitolisant hydrochloride

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Pitolisant hydrochloride Histamine Receptor antagonist

Cat.No.S5926

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 Histamine Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 332.31

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Quality Control

Batch: S592601 DMSO]66 mg/mL]false]Water]66 mg/mL]false]Ethanol]66 mg/mL]false Purity: 99.96%
99.96

Solubility

In vitro
Batch:

DMSO : 66 mg/mL (198.6 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 66 mg/mL

Ethanol : 66 mg/mL

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 332.31 Formula

C17H27Cl2NO

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 903576-44-3 -- Storage of Stock Solutions

Synonyms Tiprolisant hydrochloride, BF-2649 HCl Smiles C1CCN(CC1)CCCOCCCC2=CC=C(C=C2)Cl.Cl

Mechanism of Action

Targets/IC50/Ki
H3 receptor
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.
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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05458128 Active not recruiting
Idiopathic Hypersomnia|Excessive Daytime Sleepiness
Harmony Biosciences LLC
 August 19 2022 Phase 3
NCT02929342 Completed
Healthy Volunteers
Bioprojet
 July 2016 Phase 1
NCT02611687 Active not recruiting
Narcolepsy With Cataplexy|Narcolepsy Without Cataplexy
Bioprojet
 June 6 2016 Phase 3

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