362665-56-3 | Pitolisant

Packsize	Purity	Availability	Price	Discounted Price
10mg	≥98%	in stock	$183.00	$128.00
25mg	≥98%	in stock	$299.00	$209.00
50mg	≥98%	in stock	$465.00	$326.00
1g	95%	in stock	$713.00	$499.00
5g	95%	in stock	$2,112.00	$1,479.00

Description

• Catalog Number: AB78400
• Chemical Name: Pitolisant
• CAS Number: 362665-56-3
• Molecular Formula: C17H26ClNO
• Molecular Weight: 295.8474
• MDL Number: MFCD18782650
• SMILES: Clc1ccc(cc1)CCCOCCCN1CCCCC1

Computed Properties

• Complexity: 235
• Covalently-Bonded Unit Count: 1
• Heavy Atom Count: 20
• Hydrogen Bond Acceptor Count: 2
• Rotatable Bond Count: 8
• XLogP3: 4.3

Literature

• The European Medicines Agency review of pitolisant for treatment of narcolepsy: summary of the scientific assessment by the Committee for Medicinal Products for Human Use.

  Sleep medicine 20170501

• Safety and efficacy of pitolisant on cataplexy in patients with narcolepsy: a randomised, double-blind, placebo-controlled trial.

  The Lancet. Neurology 20170301

• International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.

  Pharmacological reviews 20150701

• Studies on molecular properties prediction and histamine H3 receptor affinities of novel ligands with uracil-based motifs.

  European journal of medicinal chemistry 20141030

• Overdose of the histamine H₃ inverse agonist pitolisant increases thermal pain thresholds.

  Inflammation research : official journal of the European Histamine Research Society ... [et al.] 20121101

• Increasing histamine neurotransmission in Gilles de la Tourette syndrome.

  Journal of neurology 20120201

• Pitolisant, an inverse agonist of the histamine H3 receptor: an alternative stimulant for narcolepsy-cataplexy in teenagers with refractory sleepiness.

  Clinical neuropharmacology 20120101

• Novel chalcone-based fluorescent human histamine h(3) receptor ligands as pharmacological tools.

  Frontiers in systems neuroscience 20120101

• Several down, a few to go: histamine H3 receptor ligands making the final push towards the market?

  Expert opinion on investigational drugs 20111201

• Histamine H1, H3 and H4 receptors are involved in pruritus.

  Neuroscience 20110908

• Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.

  Journal of medicinal chemistry 20110714

• The histamine H3 receptor: from discovery to clinical trials with pitolisant.

  British journal of pharmacology 20110601

• Discovery of histamine H3 antagonists for the treatment of cognitive disorders and Alzheimer's disease.

  The Journal of pharmacology and experimental therapeutics 20110101

• Histaminergic mechanisms for modulation of memory systems.

  Neural plasticity 20110101

• Azole derivatives as histamine H3 receptor antagonists, part 2: C-C and C-S coupled heterocycles.

  Bioorganic & medicinal chemistry letters 20101001

• Azole derivatives as histamine H3 receptor antagonists, part I: thiazol-2-yl ethers.

  Bioorganic & medicinal chemistry letters 20101001

• Recent advances in histamine H3 receptor antagonists/inverse agonists.

  Expert opinion on therapeutic patents 20100901

• Modulation of prepulse inhibition and stereotypies in rodents: no evidence for antipsychotic-like properties of histamine H3-receptor inverse agonists.

  Psychopharmacology 20100701

• Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists.

  European journal of medicinal chemistry 20091101

• 5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity.

  Journal of medicinal chemistry 20090709

• Fluorinated non-imidazole histamine H3 receptor antagonists.

  Bioorganic & medicinal chemistry letters 20090415

• Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands.

  Bioorganic & medicinal chemistry 20090415

• Synthesis and evaluation of structurally constrained quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.

  Journal of medicinal chemistry 20081113

• Piperidine variations in search for non-imidazole histamine H(3) receptor ligands.

  Bioorganic & medicinal chemistry 20080915

• An inverse agonist of the histamine H(3) receptor improves wakefulness in narcolepsy: studies in orexin-/- mice and patients.

  Neurobiology of disease 20080401

• Histamine H3 antagonists as wake-promoting and pro-cognitive agents.

  Current topics in medicinal chemistry 20080101

• Brain histamine and schizophrenia: potential therapeutic applications of H3-receptor inverse agonists studied with BF2.649.

  Biochemical pharmacology 20070415

• BF2.649 [1-{3-[3-(4-Chlorophenyl)propoxy]propyl}piperidine, hydrochloride], a nonimidazole inverse agonist/antagonist at the human histamine H3 receptor: Preclinical pharmacology.

  The Journal of pharmacology and experimental therapeutics 20070101

• Keynote review: histamine H3 receptor antagonists reach out for the clinic.

  Drug discovery today 20051201