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BTRX-246040

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]

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
  • 1307245-86-8
ChemSpider
  • 34248711
UNII
  • 4I67US2V8Q
ChEMBL
  • ChEMBL3304244
Chemical and physical data
FormulaC22H23ClF2N4O2S
Molar mass480.96 g·mol−1
3D model (JSmol)
  • Interactive image
  • 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

See also edit

References edit

  1. ^ a b c "BTRX 246040". AdisInsight. Springer Nature Switzerland AG.
  2. ^ 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.
  3. ^ 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.
  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 edit

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

btrx, 246040, also, known, 2940094, potent, selective, nociceptin, receptor, antagonist, which, under, development, blackthorn, therapeutics, lilly, treatment, major, depressive, disorder, demonstrated, proof, concept, clinical, efficacy, depression, 2017, pha. 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 BTRX 246040Clinical dataOther namesBTRX 246040Routes ofadministrationBy mouthLegal statusLegal statusInvestigationalIdentifiersIUPAC 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 methanolCAS Number1307245 86 8ChemSpider34248711UNII4I67US2V8QChEMBLChEMBL3304244Chemical and physical dataFormulaC 22H 23Cl F 2N 4O 2SMolar mass480 96 g mol 13D model JSmol Interactive imageSMILES Cc1c cn n1 c2c cccn2 CO CN3CCC4 CC3 c5c cc s5 Cl C CO4 F FInChI 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 1H3Key NKQHBJNRBKHUQR UHFFFAOYSA NSee also editList of investigational antidepressants J 113 397 JTC 801 SB 612 111References edit a b c BTRX 246040 AdisInsight Springer Nature Switzerland AG a b Dale E Bang Andersen B Sanchez 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 nbsp This drug article relating to the nervous system is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title BTRX 246040 amp oldid 1199045419, wikipedia, wiki, book, books, library,

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