CAS 362665-56-3 Tiprolisant

Tiprolisant - CAS 362665-56-3

Catalog number: 362665-56-3

Please be kindly noted products are not for therapeutic use. We do not sell to patients.

Molecular Formula:
Molecular Formula	C17H26ClNO
Molecular Weight:
Molecular Weight	295.85
COA:
COA	Inquire
Targets:
Targets	Histamine Receptor
Description:
Description	Tiprolisant is potent and selective nonimidazole inverse agonist at the histamine H3 receptor. (Ki=0.16 nM).

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Purity:
Purity	≥95%
Appearance:
Appearance	Solid powder
Synonyms:
Synonyms	Pitolisant; 1-[3-[3-(4-chlorophenyl)propoxy]propyl]piperidine;
Solubility:
Solubility	Soluble in DMSO
Storage:
Storage	Store at -20 °C
MSDS:
MSDS	Inquire
Application:
Application	The histamine H3 receptor.
Quality Standard:
Quality Standard	Enterprise Standard
Shelf Life:
Shelf Life	As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly

Quantity:
Quantity	Milligrams-Grams
InChIKey:
InChIKey	NNACHAUCXXVJSP-UHFFFAOYSA-N
InChI:
InChI	1S/C17H26ClNO/c18-17-9-7-16(8-10-17)6-4-14-20-15-5-13-19-11-2-1-3-12-19/h7-10H,1-6,11-15H2
Canonical SMILES:
Canonical SMILES	C1CCN(CC1)CCCOCCCC2=CC=C(C=C2)Cl
Current Developer:
Current Developer	Bioprojet

1.Efficacy of the histamine 3 receptor (H3R) antagonist pitolisant (formerly known as tiprolisant; BF2.649) in epilepsy: dose-dependent effects in the human photosensitivity model.

Kasteleijn-Nolst Trenité D1, Parain D, Genton P, Masnou P, Schwartz JC, Hirsch E. Epilepsy Behav. 2013 Jul;28(1):66-70. doi: 10.1016/j.yebeh.2013.03.018. Epub 2013 May 8.

A new class of drugs, the nonimidazole histamine 3 receptor (H3R) antagonists, has been developed in the past decade for treatment of various brain diseases. Pitolisant is such a drug. We studied the pharmacodynamic effect of pitolisant in patients with epilepsy in early Phase II, using the photosensitivity proof of concept model. A total of 14 adult patients (11 females and 3 males; 5 drug naïve) were studied for three days to evaluate the effect of a single oral dose of pitolisant on EEG photosensitivity ranges. All patients showed repeatedly a generalized photoparoxysmal response (PPR) prior to drug administration on placebo Day 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). Patients on the highest dosage (60 mg) showed the strongest effect with an effect lasting up to 28 h.

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