A series of bifunctional peptides with opioid agonist and substance P antagonist bioactivities
were designed with the concept of overlapping pharmacophores. In this concept, the …

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 …

The optimization and truncation of our lead peptide-derived ligand TY005 possessing eight
amino-acid residues was performed. Among the synthesized derivatives, NP30 (Tyr 1-DAla …

Several bifunctional peptides were synthesized and characterized based on the
pentapeptide-derived ligand NP30 (1: Tyr-DAla-Gly-Phe-Gly-Trp-O-[3′, 5′-Bzl (CF 3) 2]) …

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

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 …

An alanine scan was performed on the novel κ opioid receptor (KOR) peptide ligand CJ‐
15,208 to determine which residues contribute to the potent in vivo agonist activity observed …

In order to improve metabolic stability, a ring structure with a cystine moiety was introduced
into TY027 (Tyr-d-Ala-Gly-Phe-Met-Pro-Leu-Trp-NH-[3′, 5′-(CF3) 2Bzl]), which is a lead …

A series of hydrazide-linked bifunctional peptides designed to act as agonists for δ/μ opioid
receptors and antagonists for CCK-1/CCK-2 receptors was prepared and tested for binding …

Chronic use of μ-opioid agonists has been shown to cause neurochemical adaptations
resulting in tolerance and dependence. While the analgesic effects of these drugs are …