Opioid peptides are neuromodulators that bind to opioid receptors and reduce pain
sensitivity. Endomorphins are among the most active endogenous opioid peptides, and they …

Endomorphins, the endogenous ligands of the µ-opioid receptor, are attractive candidates
for opioid-based pain-relieving agents. These tetrapeptides, with their remarkable affinity for …

Recent statistics from the World Health Organization indicate that a high percentage of
people worldwide suffer from a wide variety of acute or cancer‐associated chronic pain. At …

Endomorphins are endogenous opioid peptides in mammals and display a strong
antinociceptive effect after central administration. However, the clinical usage of these …

We synthesized two novel endomorphin-1 (EM-1) analogs by substituting the C-terminus
residue with (thienyl)-α-methylene-β-amino acids (Map). Several in vitro and in vivo assays …

Centrally acting opioids, such as morphine, are the most frequently used analgesic agents
for the treatment of severe pain. However, their usefulness is limited by the production of a …

Abstract Endomorphin (EM)-1 and EM-2 are the most effective endogenous analgesics with
efficient separation of analgesia from the risk of adverse effects. Poor metabolic stability and …

Recently we reported the synthesis and structure–activity study of endomorphin-1 (EM-1)
analogues containing novel, unnatural α-methylene-β-aminopropanoic acids (Map). In the …

Endomorphins (EMs) are potent pharmaceuticals for the treatment of pain. Herein, we
investigated several novel EM analogues with multiple modifications and oligoarginine …

Abstract Endomorphin-1 (EM1) and endomorphin-2 (EM2) are two endogenous ligands that
belong to the opioid peptide family and have the highest affinity and selectivity for the µ …