Pitolisant

Pitolisant is a nonimidazole histamine H3 receptor antagonist (Ki = 0.16 nM) and inverse agonist (EC50 = 1.5 nM). 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. When administered following reactivation, it reverses dizocilpine-induced reconsolidation deficits.Formal Name: 1-[3-[3-(4-chlorophenyl)propoxy]propyl]-piperidine, monohydrochloride. CAS Number: 903576-44-3. Synonyms: BF 2649. Molecular Formula: C17H26ClNO . HCl. Formula Weight: 332.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml, PBS (pH 7.2): 10 mg/ml. lambdamax: 221 nm. SMILES: ClC1=CC=C(CCCOCCCN2CCCCC2)C=C1.Cl. InChi Code: InChI=1S/C17H26ClNO.ClH/c18-17-9-7-16(8-10-17)6-4-14-20-15-5-13-19-11-2-1-3-12-19,/h7-10H,1-6,11-15H2,1H. InChi Key: XLFKECRRMPOAQS-UHFFFAOYSA-N.