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

Opioid receptors play an important role in both behavioral and homeostatic functions. We
herein report tetrahydroquinoline derivatives as opioid receptor antagonists. SAR studies …

For years the design of κ-opioid receptor (KOR) agonists focussed on generating yet more
potent and selective ligands that could access the CNS. As it became apparent that this …

The tropane derived compounds, 4-[(8-alkyl-8-azabicyclo [3.2. 1] octyl-3-yl)-3-arylanilino]-N,
N-diethylbenzamides (5a–d), were synthesized and found to have high affinity and …

Potent and highly selective kappa opioid receptor agonists incorporating chroman- and 2,3-dihydrobenzofuran-based
constraints - ScienceDirect Skip to main contentSkip to article Elsevier logo Journals & …

On the basis of the three-dimensional pharmacophore model of opioid κ agonists, we
simplified the structure of nalfurafine (selective κ agonist) to find the essential structural …

Molecular cloning has identified three opioid receptors: mu (MOR), delta (DOR) and kappa
(KOR). Yet, cloning of these receptor types has offered little clarification to the diverse …

2-Methyl-N-((2′-(pyrrolidin-1-ylsulfonyl) biphenyl-4-yl) methyl) propan-1-amine (PF-
04455242) is a novel κ-opioid receptor (KOR) antagonist with high affinity for human (3 nM) …

Management of moderate to severe pain by clinically used opioid analgesics is associated
with a plethora of side effects. Despite many efforts have been dedicated to reduce …

Opioid narcotics are used for the treatment of moderate-to-severe pain and primarily exert
their analgesic effects through μ receptors. Although traditional μ agonists can cause …