Pitolisant (hydrochloride)|cas 903576-44-3|DC Chemicals

Pitolisant (hydrochloride)|cas 903576-44-3|DC Chemicals

Pitolisant Hcl(BF2.649;Ciproxidine ) is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM).

IC50 Value: 0.16 nM (Ki value); 1.5 nM (EC50) [1]

Target: H3 receptor

BF2.649 behaved as a competitive antagonist with a Ki value of 0.16 nM and as an inverse agonist with an EC50 value of 1.5 nM and an intrinsic activity approximately 50% higher than that of ciproxifan.

in vitro:  BF2.649 behaved as a competitive antagonist with a Ki value of 0.16 nM and as an inverse agonist with an EC50 value of 1.5 nM and an intrinsic activity approximately 50% higher than that of ciproxifan.

Product Name: Pitolisant (hydrochloride)|Cat No: DC9465|Cas: 903576-44-3|Molecule Formular: C17H27Cl2NO|Molecule Weight: 332.3084|Other names: Pitolisant (hydrochloride)

Pitolisant Hcl(BF2.649;Ciproxidine ) is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM).
BF2.649 behaved as a competitive antagonist with a Ki value of 0.16 nM and as an inverse agonist with an EC50 value of 1.5 nM and an intrinsic activity approximately 50% higher than that of ciproxifan.
in vitro:  BF2.649 behaved as a competitive antagonist with a Ki value of 0.16 nM and as an inverse agonist with an EC50 value of 1.5 nM and an intrinsic activity approximately 50% higher than that of ciproxifan. Pitolisant in vitro potency was approximately 6 times lower at the rodent receptor.
in vivo: In mice, the oral bioavailability coefficient, i.e., the ratio of plasma areas under the curve after oral and i.v. administrations, respectively, was 84%. BF2.649 dose dependently enhanced tele-methylhistamine levels in mouse brain, an index of histaminergic neuron activity, with an ED50 value of 1.6 mg/kg p.o., a response that persisted after repeated administrations for 17 days. A statistically significant suppressive effect (standardized photosensitive response [SPR] reduction as measured with paired t-tests) for 20-, 40-, or 60-mg doses of pitolisant was seen in 9/14 (64%) patients of whom 6/14 (43%) showed abolition of the response to intermittent photic stimulation (IPS).  BF2.649 showed significant inhibitory activity in several mouse models of schizophrenia.

For research only, not for human use!