The global “opioid crisis” has placed enormous pressure on the opioid ligand discovery
community to produce novel opioid analgesics with superior opioid-related adverse-effect …

The opioids have been used for more than a thousand years and are not only the most
widely prescribed drugs for moderate to severe pain and acute pain, but also the preferred …

The addition of lithium carbenoids to isocyanates provides a versatile access to N-
substituted 2-haloacetamides: the reaction tolerates the presence of variously functionalized …

Still nowadays pain is one of the most common disabling conditions and yet it remains too
often unsolved. Analgesic opioid drugs, and mainly MOR agonists such as morphine, are …

A 3D quantitative structure-activity relationship (3D-QSAR) model for predicting the σ 2
receptor affinity has been constructed with the aim of providing a useful tool for the …

Opiate alkaloids and their synthetic derivatives are still widely used in pain management,
drug addiction, and abuse. To avoid serious side effects, compounds with properly designed …

Although persistent pain is estimated to affect about 20% of the adult population, current
treatments have poor results. Polypharmacology, which is the administration of more than …

Persistent pain states, such as those caused by nerve injury or inflammation, are associated
with altered sensations, allodynia and hyperalgesia, that are resistant to traditional …

Cyclic pentapeptide Tyr-c [D-Lys-Phe-Phe-Asp] NH 2, based on the structure of
endomorphin-2 (EM-2), which shows high affinity to the μ-opioid receptor (MOR) and a very …

The pivotal role of the stereocenter at the N-substituent of the 6, 7-benzomorphan scaffold
was investigated combining synthetic and pharmacological approaches. 2R-and 2S …