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==See also==
* [[Ketazocine]]
* [[RB-64]]
* [[ICI-199,441]]
* [[Spiradoline]]


== References ==
== References ==

Revision as of 10:35, 21 March 2023

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KSC-12-192
Clinical data
Other names"probe 1.1"
ATC code
  • None
Identifiers
  • 2-[4-(furan-2-ylmethyl)-5-[[4-methyl-3-(trifluoromethyl)phenyl]methylsulfanyl]-1,2,4-triazol-3-yl]pyridine
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
FormulaC21H17F3N4OS
Molar mass430.45 g·mol−1
3D model (JSmol)
  • CC1=C(C=C(C=C1)CSC2=NN=C(N2CC3=CC=CO3)C4=CC=CC=N4)C(F)(F)F
  • InChI=1S/C21H17F3N4OS/c1-14-7-8-15(11-17(14)21(22,23)24)13-30-20-27-26-19(18-6-2-3-9-25-18)28(20)12-16-5-4-10-29-16/h2-11H,12-13H2,1H3
  • Key:OQJGZGAYSCWFCK-UHFFFAOYSA-N

KSC-12-192 is a drug that is used in scientific research to study the κ-opioid receptor, where it acts as a biased agonist.[1]

KSC-12-192 preferentially activates G-protein coupling over β-arrestin 2 recruitment in vitro, an intrinsic activity shared with many other KOR ligands developed to separate KOR-mediated analgesia from accompanying dysphoria.

Compared with most of the known KOR G-protein biased agonists, KSC-12-192 and its parent compound ML138 have no stereoisomers.

KSC-12-192 had the highest reported potency in vitro as a KOR agonist (EC50 = 31nM) out of a range of tested compounds with the same substituted triazole scaffold.

Name(s) X R1 R2 R3
KSC-12-192 probe 1.1 O H CH3 CF3
ML138 KSC-5-240 probe 1 O H Cl Cl
KSC-12-193 probe 1.3 S H CH3 CF3
KSC-5-247G S H Cl Cl
KSC-12-238-B5 probe 1.4 O CH3 CH3 CF3
KSC-12-238-B4 O CH3 Cl Cl

See also

References

  1. ^ Zhou, Lei; Lovell, Kimberly M.; Frankowski, Kevin J.; Slauson, Stephen R.; Phillips, Angela M.; Streicher, John M.; Stahl, Edward; Schmid, Cullen L.; Hodder, Peter; Madoux, Franck; Cameron, Michael D.; Prisinzano, Thomas E.; Aubé, Jeffrey; Bohn, Laura M. (2013-12-20). "Development of functionally selective, small molecule agonists at kappa opioid receptors". The Journal of Biological Chemistry. 288 (51): 36703–36716. doi:10.1074/jbc.M113.504381. ISSN 1083-351X. PMC 3868780. PMID 24187130.{{cite journal}}: CS1 maint: unflagged free DOI (link)
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