Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 55, Issue 22, Pages 10302-10306Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm301258w
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Here we report on the design, synthesis, and biological characterization of novel kappa opioid (KOP) receptor ligands of diphenethylamines. In opioid receptor binding and functional assays, the N-cyclobutylmethyl substituted derivative 4 (HS665) showed the highest affinity and selectivity for the KOP receptor and KOP-agonist potency. Compound 4 inhibited acetic acid induced writhing after subcutaneous administration in mice via KOP receptor mediated mechanisms, being equipotent as an analgesic to the KOP agonist U50,488.
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