A histamine H3 receptor antagonist (Ki = 0.16 nM) and inverse agonist (EC50 = 1.5 nM); increases the levels of tele-methylhistamine in mouse brain (ED50 = 1.6 mg/kg); increases dopamine and acetylcholine levels in the rat prefrontal cortex at 10 mg/kg; decreases the time spent in slow wave sleep and increases the time spent awake in cats; facilitates contextual fear memory consolidation and reverses dizocilpine-induced amnesia when administered post-training at 2.5 and 5 mg/kg

Pitolisant – 50 mg

Brand:
Cayman
CAS:
903576-44-3
Storage:
-20
UN-No:
Non-Hazardous - /

Pitolisant is a nonimidazole histamine H3 receptor antagonist (Ki = 0.16 nM) and inverse agonist (EC50 = 1.5 nM).{47015} It increases the levels of tele-methylhistamine in mouse brain, indicating histaminergic neuron activity, with an ED50 value of 1.6 mg/kg. Pitolisant also increases dopamine and acetylcholine levels in the rat prefrontal cortex when administered at a dose of 10 mg/kg. It decreases the time spent in slow wave sleep and increases the time spent awake in cats. Pitolisant (2.5 and 5 mg/kg), when administered post-training, facilitates contextual fear memory consolidation and reverses dizocilpine-induced amnesia in mice.{47016} When administered following reactivation, it reverses dizocilpine-induced reconsolidation deficits.  

 

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Description

A histamine H3 receptor antagonist (Ki = 0.16 nM) and inverse agonist (EC50 = 1.5 nM); increases the levels of tele-methylhistamine in mouse brain (ED50 = 1.6 mg/kg); increases dopamine and acetylcholine levels in the rat prefrontal cortex at 10 mg/kg; decreases the time spent in slow wave sleep and increases the time spent awake in cats; facilitates contextual fear memory consolidation and reverses dizocilpine-induced amnesia when administered post-training at 2.5 and 5 mg/kg

Formal name: 1-[3-[3-(4-chlorophenyl)propoxy]propyl]-piperidine, monohydrochloride

Synonyms:  BF 2649

Molecular weight: 332.3

CAS: 903576-44-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Receptor Pharmacology|Inverse Agonists||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory||Research Area|Neuroscience|Behavioral Neuroscience|Sleep & Biological Rhythms

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