BTRX-246040

BTRX-246040
Clinical data
Other names	BTRX-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	1307245-86-8;
ChemSpider	34248711;
UNII	4I67US2V8Q;
ChEMBL	ChEMBL3304244;
CompTox Dashboard (EPA)	DTXSID201336137 ;
Chemical and physical data
Formula	C22H23ClF2N4O2S
Molar mass	480.96 g·mol−1
3D model (JSmol)	Interactive image;
	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]

References

^ ^a ^b ^c "BTRX 246040 - AdisInsight".
^ ^a ^b 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.
^ ^a ^b 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.
^ 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.

External links

BTRX-246040 (LY-2940094) - AdisInsight

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[AdisInsight-1] "BTRX 246040 - AdisInsight".

[DaleBang-Andersen2015-2] 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.

[Yin2015-3] 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.

[pmid26585287-4] 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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[2]

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[4]

See also

References

External links