Peptidomimetics and their applications for opioid peptide drug discovery
YS Lee - Biomolecules, 2022 - mdpi.com
Despite various advantages, opioid peptides have been limited in their therapeutic uses due
to the main drawbacks in metabolic stability, blood-brain barrier permeability, and …
to the main drawbacks in metabolic stability, blood-brain barrier permeability, and …
Peripherally acting opioid analgesics and peripherally-induced analgesia
V Martínez, R Abalo - Behavioural pharmacology, 2020 - journals.lww.com
The management of pain, particularly chronic pain, is still an area of medical need. In this
context, opioids remain a gold standard for the treatment of pain. However, significant side …
context, opioids remain a gold standard for the treatment of pain. However, significant side …
Multitargeted opioid ligand discovery as a strategy to retain analgesia and reduce opioid-related adverse effects
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 …
community to produce novel opioid analgesics with superior opioid-related adverse-effect …
Synthesis and structure–activity relationships of 5′-aryl-14-alkoxypyridomorphinans: Identification of a μ opioid receptor agonist/δ opioid receptor antagonist ligand …
We previously identified a pyridomorphinan (6, SRI-22138) possessing a 4-chlorophenyl
substituent at the 5′-position on the pyridine and a 3-phenylpropoxy at the 14-position of …
substituent at the 5′-position on the pyridine and a 3-phenylpropoxy at the 14-position of …
Antinociceptive efficacy of the µ-opioid/nociceptin peptide-based hybrid KGNOP1 in inflammatory pain without rewarding effects in mice: An experimental assessment …
M Dumitrascuta, M Bermudez, O Trovato, J De Neve… - Molecules, 2021 - mdpi.com
Opioids are the most effective analgesics, with most clinically available opioids being
agonists to the µ-opioid receptor (MOR). The MOR is also responsible for their unwanted …
agonists to the µ-opioid receptor (MOR). The MOR is also responsible for their unwanted …
Tryptophan Substitution in CJ-15,208 (cyclo[Phe-D-Pro-Phe-Trp]) Introduces δ-Opioid Receptor Antagonism, Preventing Antinociceptive Tolerance and Stress …
KH Scherrer, SO Eans, JM Medina, SN Senadheera… - Pharmaceuticals, 2023 - mdpi.com
The macrocyclic tetrapeptide CJ-15,208 (cyclo [Phe-D-Pro-Phe-Trp]) and its D-Trp isomer
exhibit kappa opioid receptor (KOR) antagonism which prevents stress-induced …
exhibit kappa opioid receptor (KOR) antagonism which prevents stress-induced …
Novel cyclic endomorphin analogues with multiple modifications and oligoarginine vector exhibit potent antinociception with reduced opioid-like side effects
Y Zhang, M Wang, S Wang, X Wang… - Journal of Medicinal …, 2021 - ACS Publications
Endomorphins (EMs) are potent pharmaceuticals for the treatment of pain. Herein, we
investigated several novel EM analogues with multiple modifications and oligoarginine …
investigated several novel EM analogues with multiple modifications and oligoarginine …
Novel endomorphin analogues CEMR‐1 and CEMR‐2 produce potent and long‐lasting antinociception with a favourable side effect profile at the spinal level
Y Zhang, S Wang, X Guo, X Liu, X Wang… - British Journal of …, 2024 - Wiley Online Library
Background and Purpose Endomorphins have shown great promise as pharmaceutics for
the treatment of pain. We have previously confirmed that novel endomorphin analogues …
the treatment of pain. We have previously confirmed that novel endomorphin analogues …
The impact of multifunctional enkephalin analogs and morphine on the protein changes in crude membrane fractions isolated from the rat brain cortex and …
H Ujcikova, YS Lee, L Roubalova, P Svoboda - Peptides, 2024 - Elsevier
Endogenous opioid peptides serve as potent analgesics through the opioid receptor (OR)
activation. However, they often suffer from poor metabolic stability, low lipophilicity, and low …
activation. However, they often suffer from poor metabolic stability, low lipophilicity, and low …
DPL: a comprehensive database on sequences, structures, sources and functions of peptide ligands
F Wang, N Li, C Wang, G Xing, S Cao, Q Xu… - Database, 2020 - academic.oup.com
Abstract DPL (http://www. peptide-ligand. cn/) is a comprehensive database of peptide
ligand (DPL). DPL1. 0 holds 1044 peptide ligand entries and provides references for the …
ligand (DPL). DPL1. 0 holds 1044 peptide ligand entries and provides references for the …