ArticleJournal of medicinal chemistry2009
Pentapeptides displaying mu opioid receptor agonist and delta opioid receptor partial agonist/antagonist properties.
Article in Journal of medicinal chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
23 citing papers in PubMed, 38 citations in OpenAlex.
- Enhanced antinociception of mixed efficacy opioid peptidomimetics through P-glycoprotein modulation.The Journal of pharmacology and experimental therapeutics · 2026Article
- Structural basis of μ-opioid receptor targeting by a nanobody antagonist.Nature communications · 2024Article
- Structural Basis of μ-Opioid Receptor-Targeting by a Nanobody Antagonist.bioRxiv : the preprint server for biology · 2023Article
- Peptidomimetics and Their Applications for Opioid Peptide Drug Discovery.Biomolecules · 2022Review
- Antinociceptive activity of thiazole-containing cyclized DAMGO and Leu-(Met) enkephalin analogs.Organic & biomolecular chemistry · 2019Article
- Novel Cyclic Biphalin Analogues by Ruthenium-Catalyzed Ring Closing Metathesis:ACS medicinal chemistry letters · 2019Article
- In vivo effects of μ-opioid receptor agonist/δ-opioid receptor antagonist peptidomimetics following acute and repeated administration.British journal of pharmacology · 2018Article
- Fentanyls continue to replace heroin in the drug arena: the cases of ocfentanil and carfentanil.Forensic toxicology · 2018Review
- The behavioral effects of a mixed efficacy antinociceptive peptide, VRP26, following chronic administration in mice.Psychopharmacology · 2016Article
- Cyclic Opioid Peptides.Current medicinal chemistry · 2016Review
- Isocyanide-Based Multicomponent Reactions for the Synthesis of Heterocycles.Molecules (Basel, Switzerland) · 2015Review
- Rapid Synthesis of Boc-2',6'-dimethyl-l-tyrosine and Derivatives and Incorporation into Opioid Peptidomimetics.ACS medicinal chemistry letters · 2015Article
- Further Optimization and Evaluation of Bioavailable, Mixed-Efficacy μ-Opioid Receptor (MOR) Agonists/δ-Opioid Receptor (DOR) Antagonists: Balancing MOR and DOR Affinities.Journal of medicinal chemistry · 2015Article
- Synthesis of Carfentanil Amide Opioids Using the Ugi Multicomponent Reaction.ACS chemical neuroscience · 2015Article
- Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines.ACS medicinal chemistry letters · 2015Article
- Development of a bioavailable μ opioid receptor (MOPr) agonist, δ opioid receptor (DOPr) antagonist peptide that evokes antinociception without development of acute tolerance.Journal of medicinal chemistry · 2014Article
- Translation of structure-activity relationships from cyclic mixed efficacy opioid peptides to linear analogues.Biopolymers · 2014Article
- The role of imidazole in peptide cyclization by transesterification: parallels to the catalytic triads of serine proteases.Organic & biomolecular chemistry · 2013Article
- Opioid peptidomimetics: leads for the design of bioavailable mixed efficacy μ opioid receptor (MOR) agonist/δ opioid receptor (DOR) antagonist ligands.Journal of medicinal chemistry · 2013Article
- Variation of the net charge, lipophilicity, and side chain flexibility in Dmt(1)-DALDA: Effect on Opioid Activity and Biodistribution.Journal of medicinal chemistry · 2012Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 2 countries.
Funding
Abstract
Chronic use of mu-opioid agonists has been shown to cause neurochemical adaptations resulting in tolerance and dependence. While the analgesic effects of these drugs are mediated by mu-opioid receptors (MOR), several studies have shown that antagonism or knockdown of delta-opioid receptors (DOR) can lessen or prevent development of tolerance and dependence. On the basis of computational modeling of putative active and inactive conformations of MOR and DOR, we have synthesized a series of pentapeptides with the goal of developing a MOR agonist/DOR antagonist peptide with similar affinity at both receptors as a tool to probe functional opioid receptor interaction(s). The eight resulting naphthylalanine-substituted cyclic pentapeptides displayed variable mixed-efficacy profiles. The most promising peptide (9; Tyr-c(S-CH(2)-S)[D-Cys-Phe-2-Nal-Cys]NH(2)) displayed a MOR agonist and DOR partial agonist/antagonist profile and bound with equipotent affinity (K(i) approximately 0.5 nM) to both receptors, but also showed kappa opioid receptor (KOR) agonist activity.
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What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.