Opioid agonists are well-established analgesics, widely prescribed for acute but also
chronic pain. However, their efficiency comes with the price of drastically impacting side …

A screening of conformationally constrained aromatic amino acids as base cores for the
preparation of new NK1 receptor antagonists resulted in the discovery of three new NK1 …

Herein, the synthesis and biological evaluation of dual opioid agonists–neurokinin 1
receptor (NK1R) antagonists is described. In these multitarget ligands, the two …

A reported mixed opioid agonist–neurokinin 1 receptor (NK1R) antagonist 4 (Dmt-D-Arg-
Aba-Gly-(3′, 5′-(CF 3) 2) NMe-benzyl) was modified to identify important features in both …

Multifunctional ligands with agonist bioactivities at μ/δ opioid receptors (MOR/DOR) and
antagonist bioactivity at the neurokinin-1 receptor (NK1R) have been designed and …

Morphine, which acts through opioid receptors, is one of the most efficient analgesics for the
alleviation of severe pain. However, its usefulness is limited by serious side effects …

Multivalent ligands with δ/μ opioid agonist and NK1 antagonist activities have shown
promising analgesic potency without detectable sign of toxicities, including motor skill …

The lower efficacy of opioids in neuropathic pain may be due to the increased activity of
pronociceptive systems such as substance P. We present evidence to support this …

The neurokinins are indisputably essential neurotransmitters in numerous pathoand
physiological events. Being widely distributed in the Central Nervous System (CNS) and …

A series of bifunctional peptides that act as agonists for δ and μ opioid receptors with δ
selectivity and as antagonist for neurokinin-1 (NK1) receptors were designed and …