Sigma receptors are classified into sigma1 and sigma2 subtypes. These subtypes display a
different tissue distribution and a distinct physiological and pharmacological profile in the …

Opioid analgesics are highly effective painkillers for the treatment of moderate or severe
pain, but they are associated with a number of undesirable adverse effects, including the …

Though efficacious in managing chronic, severe pain, opioid analgesics are accompanied
by significant adverse effects including constipation, tolerance, dependence, and respiratory …

A large set of tetrahydro-2-benzazepines with an α-hydroxy or α-(aryl) alkoxy substituted
benzyl moiety in the 5-position was prepared according to the recently reported C6C1+ C3N …

Here, we describe the optimization, synthesis, and associated pharmacological analgesic
activities of a new series of bifunctional piperidinamide derivatives as sigma-1 receptor (σ 1 …

Abstract The oxa‐Pictet–Spengler cyclization is the oxygen variation of the Pictet–Spengler
reaction, in which an aromatic alcohol component (generally a β‐arylethyl alcohol) reacts …

Abstract cis-N-Substituted N-normetazocine enantiomers possess peculiar pharmacological
profiles. Indeed, dextro enantiomers bind with high affinity σ 1 receptor while opposite …

Although opioids and nonsteroidal anti-inflammatory drugs (NSAIDs) are the most common
drugs used in persistent pain treatment; they have shown many side effects. The …

As a continuation of our earlier study (J. Med. Chem. 1992, 35, 4334-4343) we
conformationally restricted the-receptor ligand 2-(l-pyrrolidinyl)-JV-[2-(3, 4-dichlorophenyl) …

5-Pyrrolidinyl substituted perhydroquinoxalines were designed as conformationally
restricted κ-opioid receptor agonists restricted to the periphery. The additional N atom of the …