Tiprolisant - CAS 362665-56-3
Catalog number: 362665-56-3
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C17H26ClNO
Molecular Weight:
295.85
COA:
Inquire
Targets:
Histamine Receptor
Description:
Tiprolisant is potent and selective nonimidazole inverse agonist at the histamine H3 receptor. (Ki=0.16 nM).
Purity:
≥95%
Appearance:
Solid powder
Synonyms:
Pitolisant; 1-[3-[3-(4-chlorophenyl)propoxy]propyl]piperidine;
Solubility:
Soluble in DMSO
Storage:
Store at -20 °C
MSDS:
Inquire
Application:
The histamine H3 receptor.
Quality Standard:
Enterprise Standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
InChIKey:
NNACHAUCXXVJSP-UHFFFAOYSA-N
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:
C1CCN(CC1)CCCOCCCC2=CC=C(C=C2)Cl
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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CAS 362665-56-3 Tiprolisant

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