Home Neuronal Signaling Histamine Receptor antagonist Pitolisant hydrochloride For research use only.

Pitolisant hydrochloride

Synonyms: Tiprolisant hydrochloride, BF-2649 HCl

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

Pitolisant hydrochloride Chemical Structure

CAS No. 903576-44-3

Purity & Quality Control

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

Pitolisant hydrochloride Related Products

Signaling Pathway

Histamine Receptor Signaling Pathways

Histamine Receptor Signaling Pathway

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
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 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].
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

Chemical Information & Solubility

Molecular Weight 332.31 Formula

C17H27Cl2NO
CAS No. 903576-44-3 SDF --
Smiles C1CCN(CC1)CCCOCCCC2=CC=C(C=C2)Cl.Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 66 mg/mL ( (198.6 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 66 mg/mL

Ethanol : 66 mg/mL


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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