| 词条 | BTRX-246040 |
| 释义 |
| Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = [2-[4-[(2-chloro-4,4-difluoro-spiro[5H-thieno[2,3-c]pyran-7,4'-piperidine]-1'-yl)methyl]-3-methyl-pyrazol-1-yl]-3-pyridyl]methanol | image = LY-2940094.svg | width = 150px | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = Investigational | routes_of_administration = By mouth | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = | CAS_number = 1307245-86-8 | CAS_supplemental = | ATC_prefix = | ATC_suffix = | PubChem = | DrugBank_Ref = | DrugBank = | ChemSpiderID_Ref = | ChemSpiderID = 34248711 | ChEMBL = 3304244 | synonyms = BTRX-246040 | C=22 | H=23 | N=4 | O=2 | S=1 | Cl=1 | F=2 | SMILES = Cc1c(cn(n1)c2c(cccn2)CO)CN3CCC4(CC3)c5c(cc(s5)Cl)C(CO4)(F)F | StdInChI = 1S/C22H23ClF2N4O2S/c1-14-16(11-29(27-14)20-15(12-30)3-2-6-26-20)10-28-7-4-21(5-8-28)19-17(9-18(23)32-19)22(24,25)13-31-21/h2-3,6,9,11,30H,4-5,7-8,10,12-13H2,1H3 | StdInChIKey = NKQHBJNRBKHUQR-UHFFFAOYSA-N }}BTRX-246040, also known as LY-2940094, is a potent and selective nociceptin receptor antagonist which is under development by BlackThorn Therapeutics and Eli Lilly for the treatment of major depressive disorder (MDD).[1][2][3] It has demonstrated proof-of-concept clinical efficacy for depression.[4] As of 2017, it is in phase II clinical trials for the treatment of MDD.[1][2][3] It was also under investigation for the treatment of alcoholism, and similarly reached phase II clinical studies for this indication, but development was discontinued.[1] See also
References1. ^1 2 https://adisinsight.springer.com/drugs/800033400 2. ^1 {{cite journal|last1=Dale|first1=Elena|last2=Bang-Andersen|first2=Benny|last3=Sánchez|first3=Connie|title=Emerging mechanisms and treatments for depression beyond SSRIs and SNRIs|journal=Biochemical Pharmacology|volume=95|issue=2|year=2015|pages=81–97|issn=0006-2952|doi=10.1016/j.bcp.2015.03.011|url=http://ac.els-cdn.com/S0006295215001562/1-s2.0-S0006295215001562-main.pdf?_tid=f417c406-fa7f-11e4-8069-00000aacb35e&acdnat=1431638999_2432ab0a8c2b11b51e25962a430aee96|pmid=25813654}} 3. ^1 {{cite journal|last1=Yin|first1=Xin|last2=Guven|first2=Nuri|last3=Dietis|first3=Nikolas|title=Opioids in Depression: Not Quite There Yet|journal=UK Journal of Pharmaceutical and Biosciences|volume=3|issue=1|year=2015|pages=12–17|issn=|doi=|url=https://www.researchgate.net/profile/Nikolas_Dietis/publication/273694299_Opioids_in_Depression_Not_Quite_There_Yet/links/5508c91a0cf27e990e0ce086.pdf}} 4. ^{{cite journal | vauthors = Post A, Smart TS, Krikke-Workel J, Dawson GR, Harmer CJ, Browning M, Jackson K, Kakar R, Mohs R, Statnick M, Wafford K, McCarthy A, Barth V, Witkin JM | title = A Selective Nociceptin Receptor Antagonist to Treat Depression: Evidence from Preclinical and Clinical Studies | journal = Neuropsychopharmacology | volume = | issue = | pages = | year = 2015 | pmid = 26585287 | doi = 10.1038/npp.2015.348 | url = }} External links
2 : Nociceptin receptor antagonists|Synthetic opioids |
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