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;
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[edit]

^ ^a ^b ^c "BTRX 246040". AdisInsight. Springer Nature Switzerland AG.
^ ^a ^b Dale 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.
^ ^a ^b Yin 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.
^ 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[edit]

"BTRX-246040 (LY-2940094)". AdisInsight. Springer Nature Switzerland AG.

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[AdisInsight-1] "BTRX 246040". AdisInsight. Springer Nature Switzerland AG.

[DaleBang-Andersen2015-2] Dale 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.

[Yin2015-3] Yin 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.

[pmid26585287-4] 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.

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