209808-18-4Relevant articles and documents
Tuned-affinity bivalent ligands for the characterization of opioid receptor heteromers
Harvey, Jessica H.,Long, Darcie H.,Whistler, Jennifer L.,England, Pamela M.
, p. 640 - 644,5 (2020/08/31)
Opioid receptors, including the μ- and δ-opioid receptors (MOR and DOR), are important targets for the treatment of pain. Although there is mounting evidence that these receptors form heteromers, the functional role of the MOR/DOR heteromer remains unresolved. We have designed and synthesized bivalent ligands as tools to elucidate the functional role of the MOR/DOR heteromer. Our ligands (L2 and L4) are comprised of a compound with low affinity at the DOR tethered to a compound with high affinity at the MOR, with the goal of producing ligands with "tuned affinity" at MOR/DOR heteromers as compared to DOR homomers. Here, we show that both L2 and L4 demonstrate enhanced affinity at MOR/DOR heteromers as compared to DOR homomers, thereby providing unique pharmacological tools to dissect the role of the MOR/DOR heteromer in pain.
DIARYLMETHYLIDENE PIPERIDINE DERIVATIVES, PREPARATIONS THEREOF AND USES THEREOF
-
Page/Page column 18; 31, (2010/02/12)
Compounds of Formula: wherein R1, R2, and R3 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in p
DIARYLMETHYLIDENE PIPERIDINE DERIVATIVES, PREPARATIONS THEREOF AND USES THEREOF
-
Page 34, (2008/06/13)
Compounds of general formula: wherein R1, R2, R3, R4, and R5 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prep
