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.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Histamine Receptor Products


CAS 83881-52-1 Cetirizine diHCl

Cetirizine diHCl
(CAS: 83881-52-1)

Cetirizine is a major metabolite of hydroxyzine, and a racemic selective H1 receptor antagonist.

CAS 90729-42-3 Carebastine

Carebastine
(CAS: 90729-42-3)

Carebastine is the active first-pass metabolite of Ebastine. Carebastine acts as a selective histamine H1 receptor antagonist that has the potential for allergy...

CAS 523-87-5 Dramamine

Dramamine
(CAS: 523-87-5)

Dimenhydrinate is an over-the-counter antiemetic used to prevent nausea and motion sicknes composed of 8-Chlorotheophylline and Diphenhydramine.

CAS 149629-70-9 Impentamine dihydrobromide

Impentamine dihydrobromide
(CAS: 149629-70-9)

Impentamine dihydrobromide is the dihydrobromide salt of impentamine, which is a highly selective and the most potent histamine H3 antagonist with pA2 value of ...

CAS 79794-75-5 Loratadine

Loratadine
(CAS: 79794-75-5)

Loratadine is a histamine H1 receptor antagonist, used to treat allergies. It also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM.

CAS 869497-75-6 JNJ 10191584 maleate

JNJ 10191584 maleate
(CAS: 869497-75-6)

The maleate salt form of JNJ 10191584, which has been found to be a selective histamine H4 receptor silent antagonist and could restrain mast cell and eosinophi...

CAS 5636-83-9 Dimethindene

Dimethindene
(CAS: 5636-83-9)

Dimethindene is a selective histamine H1 antagonist. It binds to the histamine H1 receptor. It is an antiallergic drug and is used in hypersensitivity reactions...

CAS 195867-54-0 HTMT dimaleate

HTMT dimaleate
(CAS: 195867-54-0)

HTMT dimaleate is a histamine H1 and H2 receptor agonist with 4x104 fold activity over histamine in H2-mediated effects in natural suppressor cells. HTMT dimale...

Chemical Structure

CAS 362665-56-3 Tiprolisant

Quick Inquiry

Verification code

Featured Items