Catalog No.S5926 Synonyms: Tiprolisant hydrochloride, BF-2649 HCl
Molecular Weight(MW): 332.31
Pitolisant 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.
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|Description||Pitolisant 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 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.|
|In vitro||DMSO||66 mg/mL (198.6 mM)|
|Water||66 mg/mL (198.6 mM)|
|Ethanol||66 mg/mL (198.6 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||Tiprolisant hydrochloride, BF-2649 HCl|
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