Cargando…

Development of a Bioavailable μ Opioid Receptor (MOPr) Agonist, δ Opioid Receptor (DOPr) Antagonist Peptide That Evokes Antinociception without Development of Acute Tolerance

[Image: see text] We have previously described a cyclic tetrapeptide, 1, that displays μ opioid receptor (MOPr) agonist and δ opioid receptor (DOPr) antagonist activity, a profile associated with a reduced incidence of opioid tolerance and dependence. Like many peptides, 1 has poor bioavailability....

Descripción completa

Detalles Bibliográficos
Autores principales:	Mosberg, Henry I., Yeomans, Larisa, Anand, Jessica P., Porter, Vanessa, Sobczyk-Kojiro, Katarzyna, Traynor, John R., Jutkiewicz, Emily M.
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	American Chemical Society 2014
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3993928/ https://www.ncbi.nlm.nih.gov/pubmed/24641190 http://dx.doi.org/10.1021/jm5002088

Ejemplares similares

Effects of N-Substitutions on the Tetrahydroquinoline (THQ) Core of Mixed-Efficacy μ-Opioid Receptor (MOR)/δ-Opioid Receptor (DOR) Ligands
por: Harland, Aubrie A., et al.
Publicado: (2016)

LP1 and LP2: Dual-Target MOPr/DOPr Ligands as Drug Candidates for Persistent Pain Relief
por: Pasquinucci, Lorella, et al.
Publicado: (2021)

The Possible Role of MOPr-DOPr Heteromers and Its Regulatory Protein RTP4 at Sensory Neurons in Relation to Pain Perception
por: Fujita, Wakako
Publicado: (2020)

The Multimodal MOPr/DOPr Agonist LP2 Reduces Allodynia in Chronic Constriction Injured Rats by Rescue of TGF-β1 Signalling
por: Fidilio, Annamaria, et al.
Publicado: (2021)

Role of protein kinase C and μ-opioid receptor (MOPr) desensitization in tolerance to morphine in rat locus coeruleus neurons
por: Bailey, C P, et al.
Publicado: (2009)

Ligand‐specific recycling profiles determine distinct potential for chronic analgesic tolerance of delta‐opioid receptor (DOPr) agonists
por: Bagheri Tudashki, Hanieh, et al.
Publicado: (2020)

Selectively Promiscuous Opioid Ligands: Discovery of High Affinity/Low Efficacy Opioid Ligands with Substantial Nociceptin Opioid Peptide Receptor Affinity
por: Kumar, Vinod, et al.
Publicado: (2014)

Negative modulation of spinal κ-opioid receptor-mediated antinociception by the µ-opioid receptor at selective doses of (−)-pentazocine
por: Robinson, Douglas L., et al.
Publicado: (2018)

δ-opioid Receptor, Microglia and Neuroinflammation
por: Xu, Yuan, et al.
Publicado: (2023)

Placement of Hydroxy Moiety on Pendant of Peptidomimetic Scaffold Modulates Mu and Kappa Opioid Receptor Efficacy
por: Harland, Aubrie A., et al.
Publicado: (2017)

Structure of the δ-opioid receptor bound to naltrindole
por: Granier, Sébastien, et al.
Publicado: (2012)

Activation profiles of opioid ligands in HEK cells expressing δ opioid receptors
por: Gharagozlou, Parham, et al.
Publicado: (2002)

Clinical opioids differentially induce co-internalization of μ- and δ-opioid receptors
por: Bao, Fenghua, et al.
Publicado: (2018)

Chronic Ethanol Consumption in Rats Produces Opioid Antinociceptive Tolerance through Inhibition of Mu Opioid Receptor Endocytosis
por: He, Li, et al.
Publicado: (2011)

The Sigma 2 receptor promotes and the Sigma 1 receptor inhibits mu-opioid receptor-mediated antinociception
por: Sánchez-Blázquez, Pilar, et al.
Publicado: (2020)

Roles of Opioid Receptor Subtype in the Spinal Antinociception of Selective Cyclooxygenase 2 Inhibitor
por: Choi, Cheol Hun, et al.
Publicado: (2010)

Hair Growth Promotion by δ-Opioid Receptor Activation
por: Zheng, Mei, et al.
Publicado: (2021)

(-)-Pentazocine induces visceral chemical antinociception, but not thermal, mechanical, or somatic chemical antinociception, in μ-opioid receptor knockout mice
por: Ide, Soichiro, et al.
Publicado: (2011)

Opioids drive breast cancer metastasis through the δ-opioid receptor and oncogenic STAT3
por: Tripolt, Sabrina, et al.
Publicado: (2021)

Oxytocin Is a Positive Allosteric Modulator of κ-Opioid Receptors but Not δ-Opioid Receptors in the G Protein Signaling Pathway
por: Miyano, Kanako, et al.
Publicado: (2021)

δ-Opioid Receptor as a Molecular Target for Increasing Cardiac Resistance to Reperfusion in Drug Development
por: Naryzhnaya, Natalia V., et al.
Publicado: (2023)

Antinociceptive Effects of Cardamonin in Mice: Possible Involvement of TRPV(1), Glutamate, and Opioid Receptors
por: Ping, Chung Pui, et al.
Publicado: (2018)

PM287. Mixtures of opioid receptor agonists and cannabinoid receptor agonists: enhanced antinociception without abuse liability
por: France, Charles P, et al.
Publicado: (2016)

Antinociceptive Action of Isolated Mitragynine from Mitragyna Speciosa through Activation of Opioid Receptor System
por: Shamima, Abdul Rahman, et al.
Publicado: (2012)

Antinociceptive effects of dehydrocorydaline in mouse models of inflammatory pain involve the opioid receptor and inflammatory cytokines
por: Yin, Zhi-Yu, et al.
Publicado: (2016)

The antinociceptive effects of ferulic acid on neuropathic pain: involvement of descending monoaminergic system and opioid receptors
por: Xu, Ying, et al.
Publicado: (2016)

The novel μ‐opioid receptor agonist PZM21 depresses respiration and induces tolerance to antinociception
por: Hill, Rob, et al.
Publicado: (2018)

In vivo antinociception of potent mu opioid agonist tetrapeptide analogues and comparison with a compact opioid agonist - neurokinin 1 receptor antagonist chimera
por: Guillemyn, Karel, et al.
Publicado: (2012)

Synthesis and Pharmacological Activities of 6-Glycine Substituted 14-Phenylpropoxymorphinans, a Novel Class of Opioids with High Opioid Receptor Affinities and Antinociceptive Potencies
por: Spetea, Mariana, et al.
Publicado: (2011)

Antidepressant-like Effects of δ Opioid Receptor Agonists in Animal Models
por: Saitoh, Akiyoshi, et al.
Publicado: (2012)

Inhibition of Activity of GABA Transporter GAT1 by δ-Opioid Receptor
por: Pu, Lu, et al.
Publicado: (2012)

Exploring Binding Properties of Agonists Interacting with a δ-Opioid Receptor
por: Collu, Francesca, et al.
Publicado: (2012)

Structural basis for bifunctional peptide recognition at human δ-Opioid receptor
por: Fenalti, Gustavo, et al.
Publicado: (2015)

δ-Opioid Receptors, microRNAs, and Neuroinflammation in Cerebral Ischemia/Hypoxia
por: Chen, Yi-Meng, et al.
Publicado: (2020)

δ-Opioid receptor as a potential therapeutic target for ischemic stroke
por: Subedi, Kalpana, et al.
Publicado: (2019)

Opioids in cancer: The κ-opioid receptor
por: Zhou, Qier, et al.
Publicado: (2022)

Nitro-benzylideneoxymorphone, a bifunctional mu and delta opioid receptor ligand with high mu opioid receptor efficacy
por: Olson, Keith M., et al.
Publicado: (2023)

Synthesis, purification, characterization, and antinociceptive activity of opioids peptides
por: Nóbrega, Mariana, et al.
Publicado: (2014)

Peripheral Antinociception Induced by Aripiprazole Is Mediated by the Opioid System
por: Ferreira, Renata Cristina Mendes, et al.
Publicado: (2017)

A Genetic Screen To Assess Dopamine Receptor (DopR1) Dependent Sleep Regulation in Drosophila
por: Jiang, Yiqin, et al.
Publicado: (2016)

Cannot write session to /tmp/vufind_sessions/sess_1vnc29cf0l6chlpdlbkc4juldj