| 词条 | Pitolisant |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 464208162 | IUPAC_name = 1-[3-[3-(4-chlorophenyl)propoxy]propyl]piperidine | image = Pitolisant skeletal.svg | width = 250px | tradename = Wakix | pregnancy_AU = | pregnancy_US = | pregnancy_category = | licence_EU = yes | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = Oral | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = {{cascite|changed|??}} | CAS_number = 362665-56-3 | CAS_supplemental = 903576-44-3 (hydrochloride) 362665-57-4 (oxalate) | class = Histamine H3 receptor inverse agonists | ATC_prefix = N07 | ATC_suffix = XX11 | ATC_supplemental = | PubChem = 9948102 | IUPHAR_ligand = | DrugBank_Ref = | DrugBank = | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 8123714 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 4BC83L4PIY | KEGG_Ref = {{keggcite|changed|kegg}} | KEGG = D10749 | ChEBI_Ref = {{ebicite|correct|EBI}} | ChEBI = 134709 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 462605 | synonyms = Tiprolisant; Ciproxidine; BF2.649 | C=17 | H=26 | Cl=1 | N=1 | O=1 | molecular_weight = 295.851 g/mol | SMILES = C1CCN(CC1)CCCOCCCC2=CC=C(C=C2)Cl | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 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 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = NNACHAUCXXVJSP-UHFFFAOYSA-N }}Pitolisant ({{abbrlink|INN|International Nonproprietary Name}}), also known as tiprolisant ({{abbrlink|USAN|United States Adopted Name}}) .[1] Pitolisant is an investigational medication in the U.S. that is not approved by the FDA. It was granted orphan designation for the treatment of narcolepsy, Fast Track designation for the treatment of excessive daytime sleepiness (EDS) and cataplexy in patients with narcolepsy, and Breakthrough Therapy designation for the treatment of cataplexy in patients with narcolepsy. Pitolisant, a first-in-class medication, is a potent and highly selective histamine 3 (H₃) receptor antagonist/inverse agonist; it enhances the activity of histaminergic neurons in the brain that function to improve a patient’s wakefulness and inhibit attacks of cataplexy. It was designed and developed by Bioprojet, who has marketed the product in Europe since its approval by the European Medicines Agency in 2016. Harmony’s goal is to obtain FDA approval to market this new medication in the U.S. in 2019. If approved, pitolisant would represent the first new therapy in the U.S. in over 15 years for the treatment of both EDS and cataplexy in adult patients with narcolepsy. The NDA (New Drug Submission), submission is based on results from the clinical development program in narcolepsy, which included over 300 patients, some of whom were treated for up to five years. It also included safety data in over 1500 patients across multiple patient populations. [https://www.harmonybiosciences.com/newsroom/harmony-biosciences-announces-file-acceptance-of-its-new-drug-application/] It was developed by Jean-Charles Schwartz, Walter Schunack, and colleagues after the former discovered the H3 receptor.[2] It was the first H3 receptor inverse agonist to be tested in humans or introduced for clinical use.[2] References1. ^http://adisinsight.springer.com/drugs/800029451 2. ^1 {{cite journal | vauthors = Schwartz JC | title = The histamine H3 receptor: from discovery to clinical trials with pitolisant | journal = Br. J. Pharmacol. | volume = 163 | issue = 4 | pages = 713–21 | year = 2011 | pmid = 21615387 | pmc = 3111674 | doi = 10.1111/j.1476-5381.2011.01286.x | url = }} External links
5 : Chloroarenes|Ethers|H3 receptor antagonists|Piperidines|Stimulants |
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