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| | Tiprolisant oxalate Basic information |
| Product Name: | Tiprolisant oxalate | | Synonyms: | Pitolisant (oxalate);Tiprolisant oxalate;1-[3-[3-(4-Chlorophenyl)propoxy]propyl]piperidine ethanedioate (1:1);Pitolisant ethanedioate (1:1) | | CAS: | 362665-57-4 | | MF: | C19H28ClNO5 | | MW: | 385.88232 | | EINECS: | | | Product Categories: | | | Mol File: | 362665-57-4.mol |  |
| | Tiprolisant oxalate Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO : 50 mg/mL (129.57 mM; Need ultrasonic) | | form | Powder | | color | Off-white to light yellow |
| | Tiprolisant oxalate Usage And Synthesis |
| Uses | Pitolisant oxalate is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM). | | in vivo | The administration of Pitolisantat a single dose of 10 mg/kg 30 min before a single dose of Olanzapine (2 mg/kg b.w.) also significantly affects immobility time in the FST. Subsequent administration of the aforementioned drug sequence in mice statistically significantly increases the duration of immobility in comparison to the time determined in the control group in the FST. It decreased locomotor activity as well. In contrast, the results obtained in subchronic treatment after fifteen administrations of both drugs (Pitolisant 10 mg/kg b.w., and after 30 min Olanzapine 2 mg/kg b.w., and again after 4 h Olanzapine 2 mg/kg b.w.) show that the administration of Pitolisant followed by that of Olanzapine equalized the locomotor activity in mice; in comparison to the level of motility in the control group, to which only Pitolisant is administered. More importantly, this combination of drugs significantly reduces immobility time to the level obtained in the control group in the forced swim test in mice [one-way ANOVA; F (3,20)=4.226,P=0.0181][2]. Rats given Pitolisant (10 mg/kg) during the conditioning phase stayed 502±94 s on the paired texture, a value not statistically different from that of controls, indicating that Pitolisant did not support place preference[3]. | | References | [1] Ligneau X, et al. BF2.649 [1-{3-[3-(4-Chlorophenyl)propoxy]propyl}piperidine, hydrochloride], a nonimidazole inverse agonist/antagonist at the human histamine H3 receptor: Preclinical pharmacology. J Pharmacol Exp Ther. 2007 Jan;320(1):365-75. DOI:10.1124/jpet.106.111039
[2] Dudek M, et al. H3 histamine receptor antagonist pitolisant reverses some subchronic disturbances induced by olanzapine in mice. Metab Brain Dis. 2016 Oct;31(5):1023-9. DOI:10.1007/s11011-016-9840-z
[3] Uguen M, et al. Preclinical evaluation of the abuse potential of Pitolisant, a histamine H receptor inverse agonist/antagonist compared with Modafinil. Br J Pharmacol. 2013 Jun;169(3):632-44. DOI:10.1111/bph.12149 |
| | Tiprolisant oxalate Preparation Products And Raw materials |
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