BTRX-246040

BTRX-246040
Clinical data
Other namesBTRX-246040
Routes of
administration		By mouth
Legal status
Legal status
  • Investigational
Identifiers
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
CAS Number
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC22H23ClF2N4O2S
Molar mass480.96 g·mol−1
3D model (JSmol)
SMILES
  • Cc1c(cn(n1)c2c(cccn2)CO)CN3CCC4(CC3)c5c(cc(s5)Cl)C(CO4)(F)F
InChI
  • InChI=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
  • Key: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

References

  1. 1 2 3 https://adisinsight.springer.com/drugs/800033400
  2. 1 2 Dale, Elena; Bang-Andersen, Benny; Sánchez, Connie (2015). "Emerging mechanisms and treatments for depression beyond SSRIs and SNRIs". Biochemical Pharmacology. 95 (2): 81–97. doi:10.1016/j.bcp.2015.03.011. ISSN 0006-2952. PMID 25813654.
  3. 1 2 Yin, Xin; Guven, Nuri; Dietis, Nikolas (2015). "Opioids in Depression: Not Quite There Yet". UK Journal of Pharmaceutical and Biosciences. 3 (1): 12–17. doi:10.20510/ukjpb/3/i1/89219.
  4. ↑ 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 (2015). "A Selective Nociceptin Receptor Antagonist to Treat Depression: Evidence from Preclinical and Clinical Studies". Neuropsychopharmacology. 41 (7): 1803–1812. doi:10.1038/npp.2015.348. PMC 4869049. PMID 26585287.



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