Biological evaluation and molecular docking studies of AA3052, a compound containing a μ-selective opioid peptide agonist DALDA and d-Phe-Phe-d-Phe-Leu-Leu …

A Kowalczyk, P Kleczkowska, M Rękawek… - European Journal of …, 2016 - Elsevier
The design of novel drugs for pain relief with improved analgesic properties and diminished
side effect induction profile still remains a challenging pursuit. Tolerance is one of the most …

De novo design, synthesis, and biological activities of high-affinity and selective non-peptide agonists of the δ-opioid receptor

S Liao, J Alfaro-Lopez, MD Shenderovich… - Journal of medicinal …, 1998 - ACS Publications
On the basis of the structure− activity relationships of δ-opioid-selective peptide ligands and
on a model of the proposed bioactive conformation for a potent and selective …

In Vitro and In Vivo Pharmacological Profiles of LENART01, a Dermorphin–Ranatensin Hybrid Peptide

N Hochrainer, P Serafin, S D'Ingiullo, A Mollica… - International Journal of …, 2024 - mdpi.com
Diverse chemical and pharmacological strategies are currently being explored to minimize
the unwanted side effects of currently used opioid analgesics while achieving effective pain …

Bifunctional peptide-based opioid agonist–nociceptin antagonist ligands for dual treatment of acute and neuropathic pain

K Guillemyn, J Starnowska, C Lagard… - Journal of medicinal …, 2016 - ACS Publications
Herein, the opioid pharmacophore H-Dmt-d-Arg-Aba-β-Ala-NH2 (7) was linked to peptide
ligands for the nociceptin receptor. Combination of 7 and NOP ligands (eg, H-Arg-Tyr-Tyr …

Truncation of the peptide sequence in bifunctional ligands with mu and delta opioid receptor agonist and neurokinin 1 receptor antagonist activities

P Nair, T Yamamoto, TM Largent-Milnes… - Bioorganic & medicinal …, 2013 - Elsevier
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 …

The search for opioid analgesics with limited tolerance liability

K Wtorek, J Piekielna-Ciesielska, T Janecki, A Janecka - Peptides, 2020 - Elsevier
Reducing the well-known side effects of opioids prescribed to treat chronic pain remains
unresolved, despite extensive research in this field. Among several options to tackle this …

Synthesis and pharmacological evaluation of hybrids targeting opioid and neurokinin receptors

K Wtorek, A Adamska-Bartłomiejczyk… - Molecules, 2019 - mdpi.com
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 …

Synthesis, modeling, and pharmacological evaluation of UMB 425, a mixed μ agonist/δ antagonist opioid analgesic with reduced tolerance liabilities

JR Healy, P Bezawada, J Shim, JW Jones… - ACS chemical …, 2013 - ACS Publications
Opioid narcotics are used for the treatment of moderate-to-severe pain and primarily exert
their analgesic effects through μ receptors. Although traditional μ agonists can cause …

[HTML][HTML] Targeting peripheral kappa opioid receptors for the treatment of chronic pain

TC Beck, TA Dix, CM Reichel - Advances in nanomedicine and …, 2019 - ncbi.nlm.nih.gov
Addiction to conventional opioid pain analgesics is a major societal problem that is
increasing at an alarming rate. New drugs to combat the effects of opioid abuse are …

A new opioid designed multiple ligand derived from the μ opioid agonist endomorphin-2 and the δ opioid antagonist pharmacophore Dmt-Tic

S Salvadori, C Trapella, S Fiorini, L Negri… - Bioorganic & medicinal …, 2007 - Elsevier
Opioid compounds with mixed μ agonist/δ antagonist properties could be used as
analgesics with low propensity to induce tolerance and dependence. Here we report the …