Pitolisant-d10

Pitolisant-d10 (Tiprolisant-d10) is deuterium labeled Pitolisant. Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM) [1].

Product Specifications

Product Name Alternative

Tiprolisant-d10

UNSPSC

12352005

Target

Histamine Receptor; Isotope-Labeled Compounds

Type

Isotope-Labeled Compounds

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling; Others

Field of Research

Neurological Disease; Endocrinology

Smiles

[2H]C1([2H])C([2H])([2H])C([2H])([2H])C([2H])([2H])C([2H])([2H])N1CCCOCCCC2=CC=C(Cl)C=C2

Molecular Formula

C17H16D10ClNO

Molecular Weight

305.91

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53 (2) :211-216.|[2]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.|[3]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.|[4]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.