Abstract κ-Opioid receptor agonists with high selectivity over the μ-opioid receptor are
attractive targets in the development of drugs for pain and pruritus. We previously reported …

Morphine and structurally-derived compounds are µ opioid receptor (µOR) agonists, and the
most effective analgesic drugs. However, their usefulness is limited by serious side effects …

'Biased'ligands of G protein-coupled receptors (GPCRs) represent a type of promising
analgesic with reduced on-target side effects. PZM21, a potent μ-opioid-receptor (μOR) …

Position 6 of the morphinan skeleton plays a key role in the μ-opioid receptor (MOR) activity
in vitro and in vivo. We describe the consequence of the 6-carbonyl group deletion in N …

Conformationally constrained bicyclic derivatives of the potent and selective K‐opioid
receptor agonist 2‐(3, 4‐dichlorophenyl)‐N‐methyl‐N‐[(1S)‐1‐phenyl‐2‐(1‐pyrrolidinyl) …

An attempt to prepare a trimer having the 1, 3, 5-trioxazatriquinane skeleton led to discovery
of a novel rearrangement reaction that afforded a compound with an oxabicyclo [3.2. 1] …

By focusing on 4, 5-epoxymorphinan, a traditional opioid skeleton but a new structure in the
opioid κ-agonist research field, and by rationally applying the 'message-address …

The design of enantiopure stereoisomers of N-2-phenylcyclopropylmethyl-substituted ortho-
c oxide-bridged phenylmorphans, the E and Z isomers of an N-cinnamyl moiety, and N …

8-Amino-2, 6-methano-3-benzazocine derivatives have been made using Pd-catalyzed
amination procedures, and their affinities for opioid receptors were assessed. The 8-amino …

Two parallel synthetic methods were developed to explore the structure–activity
relationships (SAR) of a series of potent opioid agonists. This series of tropanylidene …