ArticleBioorganic & medicinal chemistry2011
Synthesis and biological evaluation of new opioid agonist and neurokinin-1 antagonist bivalent ligands.
Article in Bioorganic & medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
What it found
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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.
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Who cites it
14 citing papers in PubMed.
- GPCR Heterodimers: Implications for Biased Signaling.Handbook of experimental pharmacology · 2026Review
- Fentanyl Structure as a Scaffold for Opioid/Non-Opioid Multitarget Analgesics.International journal of molecular sciences · 2022Review
- Novel NK1R-TargetedInternational journal of molecular sciences · 2022Article
- Efficient Synthesis of Norbuprenorphines Coupled with Enkephalins and Investigation of Their Permeability.Iranian journal of pharmaceutical research : IJPR · 2019Article
- Novel Molecular Strategies and Targets for Opioid Drug Discovery for the Treatment of Chronic Pain.The Yale journal of biology and medicine · 2017Review
- Synthesis and Investigation of Mixed μ-Opioid and δ-Opioid Agonists as Possible Bivalent Ligands for Treatment of Pain.Journal of heterocyclic chemistry · 2017Article
- Detection of Receptor Heteromerization Using In Situ Proximity Ligation Assay.Current protocols in pharmacology · 2016Article
- Combatting Synthetic Designer Opioids: A Conjugate Vaccine Ablates Lethal Doses of Fentanyl Class Drugs.Angewandte Chemie (International ed. in English) · 2016Article
- Neurokinin 1 and opioid receptors: relationships and interactions in nervous system.Translational perioperative and pain medicine · 2016Article
- G Protein-Coupled Receptor Heteromers.Annual review of pharmacology and toxicology · 2016Review
- Dual Alleviation of Acute and Neuropathic Pain by Fused Opioid Agonist-Neurokinin 1 Antagonist Peptidomimetics.ACS medicinal chemistry letters · 2015Article
- Development and characterisation of novel fentanyl-delta opioid receptor antagonist based bivalent ligands.British journal of anaesthesia · 2015Article
- Revolution in GPCR signalling: opioid receptor heteromers as novel therapeutic targets: IUPHAR review 10.British journal of pharmacology · 2014Review
- Fentanyl-related compounds and derivatives: current status and future prospects for pharmaceutical applications.Future medicinal chemistry · 2014Review
Corrections and comments
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Authors and funding
11 authors.
Funding
Abstract
Newly designed bivalent ligands-opioid agonist/NK1-antagonists have been synthesized. The synthesis of new starting materials-carboxy-derivatives of Fentanyl (1a-1c) was developed. These products have been transformed to 'isoimidium perchlorates' (2a-c). The new isoimidium perchlorates have been successfully implemented in nucleophilic addition reactions, with l-tryptophan 3,5-bis(trifluoromethyl)benzyl ester to give the target compounds-amides (3a-c). Perchlorates (2a-c) successfully undergo reactions with other nucleophiles such as alcohols, amines or hydrazines. The obtained compound 3b exhibited μ-opioid agonist activity and NK1-antagonist activity and may serve as a useful lead compound for the further design of a new series of opioid agonist/NK1-antagonist compounds.
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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.