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SR-14136

From Wikipedia, the free encyclopedia

SR-14136
Clinical data
Other namesSR14136
Drug classκ-Opioid receptor agonist
Identifiers
  • 3-[(2R,6S,9aR)-6-phenyl-2,3,4,6,7,8,9,9a-octahydro-1H-quinolizin-2-yl]-1H-benzimidazol-2-one
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
FormulaC22H25N3O
Molar mass347.462 g·mol−1
3D model (JSmol)
  • C1C[C@@H]2C[C@@H](CCN2[C@@H](C1)C3=CC=CC=C3)N4C5=CC=CC=C5NC4=O
  • InChI=1S/C22H25N3O/c26-22-23-19-10-4-5-11-21(19)25(22)18-13-14-24-17(15-18)9-6-12-20(24)16-7-2-1-3-8-16/h1-5,7-8,10-11,17-18,20H,6,9,12-15H2,(H,23,26)/t17-,18-,20+/m1/s1
  • Key:KMUYAJQKQQUKSQ-GGPKGHCWSA-N

SR-14136 is a synthetic opioid receptor agonist from the orphine series. It acts primarily as a highly potent agonist for the kappa opioid receptor, being around 10x more potent than the reference kappa agonist U-69593, and is also an agonist at the nociceptin receptor with only slightly lower potency. It has substantially weaker activity at the mu opioid receptor, at which it is a partial agonist.[1]

See also

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References

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  1. Jong L, Zaveri N, Toll L (5 January 2004). "The design and synthesis of a novel quinolizidine template for potent opioid and opioid receptor-like (ORL1, NOP) receptor ligands". Bioorganic & Medicinal Chemistry Letters. 14 (1): 181–185. doi:10.1016/j.bmcl.2003.09.068. PMC 3851569. PMID 14684324.