ArticleACS medicinal chemistry letters2014
Novel cyclic biphalin analogue with improved antinociceptive properties.
Article in ACS medicinal chemistry letters, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed.
- Dihydrokoumine, a dual-target analgesic with reduced side effects isolated from a traditional Chinese medicine.Journal of advanced research · 2025Article
- Strategic applications of methylene thioacetal bonds as disulfide surrogates in peptide drug discovery.Frontiers in chemistry · 2025Review
- Analgesic Peptides: From Natural Diversity to Rational Design.Molecules (Basel, Switzerland) · 2024Review
- Synthesis and biochemical evaluation of 17-N-beta-aminoalkyl-4,5α-epoxynormorphinans.Scientific reports · 2023Article
- Evaluation of Antimicrobial Activities against VariousMolecules (Basel, Switzerland) · 2023Article
- Rimonabant-Based Compounds Bearing Hydrophobic Amino Acid Derivatives as Cannabinoid Receptor Subtype 1 Ligands.ACS medicinal chemistry letters · 2023Article
- Discovery of κ Opioid Receptor (KOR)-Selective d-Tetrapeptides with ImprovedACS medicinal chemistry letters · 2022Article
- Biphalin-A Potent Opioid Agonist-As a Panacea for Opioid System-Dependent Pathophysiological Diseases?International journal of molecular sciences · 2021Review
- In Silico Identification of Tripeptides as Lead Compounds for the Design of KOR Ligands.Molecules (Basel, Switzerland) · 2021Article
- Antinociceptive and Cytotoxic Activity of Opioid Peptides with Hydrazone and Hydrazide Moieties at the C-Terminus.Molecules (Basel, Switzerland) · 2020Article
- Developing Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalin.ACS medicinal chemistry letters · 2020Article
- Novel Cyclic Biphalin Analogues by Ruthenium-Catalyzed Ring Closing Metathesis:ACS medicinal chemistry letters · 2019Article
- Cyclic biphalin analogues with a novel linker lead to potent agonist activities at mu, delta, and kappa opioid receptors.Bioorganic & medicinal chemistry · 2018Article
- Cyclic Biphalin Analogues Incorporating a Xylene Bridge: Synthesis, Characterization, and Biological Profile.ACS medicinal chemistry letters · 2017Article
- Opioid Receptor Activity and Analgesic Potency of DPDPE Peptide Analogues Containing a Xylene Bridge.ACS medicinal chemistry letters · 2017Article
- Structure- and conformation-activity studies of nociceptin/orphanin FQ receptor dimeric ligands.Scientific reports · 2017Article
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Authors and funding
15 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Two novel opioid analogues have been designed by substituting the native d-Ala residues in position 2,2' of biphalin with two residues of d-penicillamine or l-penicillamine and by forming a disulfide bond between the thiol groups. The so-obtained compound 9 containing d-penicillamines showed excellent μ/δ mixed receptor affinities (K i (δ) = 5.2 nM; K i (μ) = 1.9 nM), together with an efficacious capacity to trigger the second messenger and a very good in vivo antinociceptive activity, whereas product 10 was scarcely active. An explanation of the two different pharmacological behaviors of products 9 and 10 was found by studying their conformational properties.
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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.