Co-activation of μ-and δ-opioid receptors elicits tolerance to morphine-induced ventilatory depression via generation of peroxynitrite
AP Young, RB Gruber, JF Discala, WJ May… - Respiratory physiology …, 2013 - Elsevier
We determined whether pretreatment with (1) the μ-/δ-opioid receptor (μ-/δ-OR) antagonist,
naloxone,(2) the δ1, 2-OR antagonist, naltrindole, or (3) the peroxynitrite scavenger, d …
naloxone,(2) the δ1, 2-OR antagonist, naltrindole, or (3) the peroxynitrite scavenger, d …
Synthesis of CF3-containing tetrapeptide surrogates via Ugi reaction/dipolar cycloaddition sequence
DV Vorobyeva, NV Sokolova, VG Nenajdenko… - Tetrahedron, 2012 - Elsevier
A convenient synthetic pathway to novel functionalized tetrapeptides containing the 1, 2, 3-
triazole moiety is described. The target molecules were obtained by the reaction of …
triazole moiety is described. The target molecules were obtained by the reaction of …
Design, synthesis, pharmacological evaluation, and structure− activity study of novel endomorphin analogues with multiple structural modifications
This study reports on new proteolytically stable, pharmacologically active endomorphin
analogues, incorporating Dmt1, Achc2, p FPhe4, or βMePhe4 unnatural amino acids …
analogues, incorporating Dmt1, Achc2, p FPhe4, or βMePhe4 unnatural amino acids …
Synthesis of Tripeptides Containing d-Trp Substituted at the Indole Ring, Assessment of Opioid Receptor Binding and in Vivo Central Antinociception
R De Marco, A Bedini, S Spampinato… - Journal of Medicinal …, 2014 - ACS Publications
The noncationizable tripeptide Ac-d-Trp-Phe-GlyNH2 was recently proposed as a novel
minimal recognition motif for μ-opioid receptor. The introduction of different substituents …
minimal recognition motif for μ-opioid receptor. The introduction of different substituents …
Pharmacological characterization of endomorphin-2-based cyclic pentapeptides with methylated phenylalanine residues
R Perlikowska, D Malfacini, MC Cerlesi, J Piekielna… - Peptides, 2014 - Elsevier
As part of our continuing studies on the structure–activity relationships of cyclic
pentapeptides based on the structure of endomorphin-2, we report here the synthesis and …
pentapeptides based on the structure of endomorphin-2, we report here the synthesis and …
The Inverse Type II β‐Turn on D‐Trp‐Phe, a Pharmacophoric Motif for MOR Agonists
L Gentilucci, A Tolomelli, R De Marco… - …, 2011 - Wiley Online Library
Herein we propose the d‐Trp‐Phe sequence within an inverse type II β‐turn as a new kind
of pharmacophoric motif for μ‐opioid receptor (MOR) cyclopeptide agonists. Initially, we …
of pharmacophoric motif for μ‐opioid receptor (MOR) cyclopeptide agonists. Initially, we …
[HTML][HTML] Low-dose morphine elicits ventilatory excitant and depressant responses in conscious rats: Role of peripheral μ-opioid receptors
F Henderson, WJ May, RB Gruber… - Open journal of …, 2013 - ncbi.nlm.nih.gov
The systemic administration of morphine affects ventilation via a mixture of central and
peripheral actions. The aims of this study were to characterize the ventilatory responses …
peripheral actions. The aims of this study were to characterize the ventilatory responses …
Endomorphin-1 analogues (MELs) penetrate the blood–brain barrier and exhibit good analgesic effects with minimal side effects
Y Wang, X Liu, D Wang, J Yang, L Zhao, J Yu… - …, 2015 - Elsevier
Endomorphins are endogenous opioid peptides in mammals and display a strong
antinociceptive effect after central administration. However, the clinical usage of these …
antinociceptive effect after central administration. However, the clinical usage of these …
The Effect of Pro2 Modifications on the Structural and Pharmacological Properties of Endomorphin-2
A Borics, JR Mallareddy, I Timári… - Journal of medicinal …, 2012 - ACS Publications
Endomorphins (EM-1 and EM-2) are selective, high affinity agonists of the μ-opioid (MOP)
receptor, an important target in pain regulation. Their clinical use is impeded by their poor …
receptor, an important target in pain regulation. Their clinical use is impeded by their poor …
Novel endomorphin-1 analogs with C-terminal oligoarginine-conjugation display systemic antinociceptive activity with less gastrointestinal side effects
C Wang, T Qiu, Y Diao, Y Zhang, N Gu - Biochimie, 2015 - Elsevier
In recent study, in order to improve the bioavailability of endomorphin-1 (EM-1), we
designed and synthesized a series of novel EM-1 analogs by replacement of L-Pro 2 by β …
designed and synthesized a series of novel EM-1 analogs by replacement of L-Pro 2 by β …