Pitolisant oxalate

Short Summary : Nonimidazole inverse agonist

Category : Neuroscience|Histamine Receptor

Purity : 0.98

CAS Number : 362665-57-4

Formula : C19H28ClNO5

Molecular Weight : 385.88

SMILE : ClC1=CC=C(C=C1)CCCOCCCN2CCCCC2.OC(C(O)=O)=O

Solubility : Soluble in DMSO

Storage : Store at -20°C

Description : Description:
IC50 Value: 0.16 nM(Ki value); 1.5 nM(EC50) [1]
Pitolisant (BF2.649) is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human 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. Pitolisant in vitro potency was approximately 6 times lower at the rodent receptor [1].
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 [1]. 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) [2]. BF2.649 showed significant inhibitory activity in several mouse models of schizophrenia [3].
Clinical trial: HARMONYIII: Long-term, Open-label Study in Narcolepsy With BF2.649 (Pitolisant). Phase3

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