ArticleACS chemical neuroscience2017
Identification of the First Marine-Derived Opioid Receptor "Balanced" Agonist with a Signaling Profile That Resembles the Endorphins.
Article in ACS chemical neuroscience, 2017. 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, 43 citations in OpenAlex.
- Form and function of actin impacts actin health and aging.iScience · 2026Article
- New paradigm of q-CAR drug development targeting disease-specific protein conformations.npj drug discovery · 2026Review
- Can Fascaplysins Be Considered Analogs of Indolo[2,3-Marine drugs · 2025Review
- Form and function of actin impacts actin health and aging.bioRxiv : the preprint server for biology · 2025Article
- Exploring marine-derived bacterial compounds targeting the μ-opioid receptor agonists through metabolic profiling to molecular modeling.Scientific reports · 2025Article
- Investigating impacts of the mycothiazole chemotype as a chemical probe for the study of mitochondrial function and aging.GeroScience · 2024Article
- A Balancing Act: Learning from the Past to Build a Future-Focused Opioid Strategy.Annual review of physiology · 2024Review
- Endogenous and Exogenous Opioids: Role in Substance Use Disorders.Advances in neurobiology · 2024Review
- Deletion of arrestin-3 does not reduce drug-seeking behavior in a longitudinal paradigm of oral morphine self-administration.Frontiers in pharmacology · 2024Article
- Review
- A New Mild Method for Synthesis of Marine Alkaloid Fascaplysin and Its Therapeutically Promising Derivatives.Marine drugs · 2023Article
- Marine-Derived Lead Fascaplysin: Pharmacological Activity, Total Synthesis, and Structural Modification.Marine drugs · 2023Review
- Antinociceptive Effects of Aaptamine, a Sponge Component, on Peripheral Neuropathy in Rats.Marine drugs · 2023Article
- Marine Natural Products as Leads against SARS-CoV-2 Infection.Journal of natural products · 2022Article
- ELA-11 protects the heart against oxidative stress injury induced apoptosis through ERK/MAPK and PI3K/AKT signaling pathways.Frontiers in pharmacology · 2022Article
- GPCR Pharmacological Profiling of Aaptamine from the Philippine SpongeMolecules (Basel, Switzerland) · 2021Article
- Site selective C-H functionalization of Mitragyna alkaloids reveals a molecular switch for tuning opioid receptor signaling efficacy.Nature communications · 2021Article
- Unnarmicin D, an Anti-inflammatory Cyanobacterial Metabolite with δ and μ Opioid Binding Activity Discovered via a Pipeline Approach Designed to Target Neurotherapeutics.ACS chemical neuroscience · 2020Article
- Agonist-selective recruitment of engineered protein probes and of GRK2 by opioid receptors in living cells.eLife · 2020Article
- Synthesis and pharmacological characterization of ethylenediamine synthetic opioids in human μ-opiate receptor 1 (OPRM1) expressing cells.Pharmacology research & perspectives · 2019Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
11 authors at 4 institutions in 1 country.
Funding
Abstract
Opioid therapeutics are excellent analgesics, whose utility is compromised by dependence. Morphine (1) and its clinically relevant derivatives such as OxyContin (2), Vicodin (3), and Dilaudid (4) are "biased" agonists at the μ opioid receptor (OR), wherein they engage G protein signaling but poorly engage β-arrestin and the endocytic machinery. In contrast, endorphins, the endogenous peptide agonists for ORs, are potent analgesics, show reduced liability for tolerance and dependence, and engage both G protein and β-arrestin pathways as "balanced" agonists. We set out to determine if marine-derived alkaloids could serve as novel OR agonist chemotypes with a signaling profile distinct from morphine and more similar to the endorphins. Screening of 96 sponge-derived extracts followed by LC-MS-based purification to pinpoint the active compounds and subsequent evaluation of a mini library of related alkaloids identified two structural classes that modulate the ORs. These included the following: aaptamine (10), 9-demethyl aaptamine (11), demethyl (oxy)-aaptamine (12) with activity at the δ-OR (EC
Indexed as
Identifiers
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.