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BTRX-246040

From Wikipedia, the free encyclopedia
Nociceptin receptor antagonist
Pharmaceutical compound
BTRX-246040
Clinical data
Other namesBTRX-246040
Routes of
administration		By mouth
Legal status
Legal status
  • Investigational
Identifiers
  • [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
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC22H23ClF2N4O2S
Molar mass480.96 g·mol−1
3D model (JSmol)
  • Cc1c(cn(n1)c2c(cccn2)CO)CN3CCC4(CC3)c5c(cc(s5)Cl)C(CO4)(F)F
  • 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 asLY-2940094, is apotent andselectivenociceptin receptorantagonist which is under development by BlackThorn Therapeutics andEli Lilly for the treatment ofmajor depressive disorder (MDD).[1][2][3] It has demonstrated proof-of-concept clinical efficacy for depression.[4] As of 2017, it is inphase IIclinical trials for the treatment of MDD.[1][2][3] It was also under investigation for the treatment ofalcoholism, and similarly reached phase II clinical studies for this indication, but development was discontinued.[1]

See also

[edit]

References

[edit]
  1. ^abc"BTRX 246040".AdisInsight. Springer Nature Switzerland AG.
  2. ^abDale E, Bang-Andersen B, Sánchez C (May 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.PMID 25813654.
  3. ^abYin X, Guven N, Dietis N (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, et al. (June 2016)."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.

External links

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μ-opioid
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Antagonists
δ-opioid
(DOR)
Agonists
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κ-opioid
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Antagonists
Nociceptin
(NOP)
Agonists
Antagonists
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