ArticleMolecular pharmacology2013
Caged naloxone reveals opioid signaling deactivation kinetics.
Article in Molecular pharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers, 1 of them a synthesis that pooled it.
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
19 citing papers in PubMed, 1 synthesis or guideline pooled it, 34 citations in OpenAlex.
- Efficacy and safety of opioid-receptor antagonists for opioid-induced constipation: a systematic review and meta-analysis.Frontiers in pharmacology · 2025Pooled it
- Neuromodulator and neuropeptide sensors and probes for precise circuit interrogation in vivo.Science (New York, N.Y.) · 2024Review
- Article
- Review
- Human OPRM1 and murine Oprm1 promoter driven viral constructs for genetic access to μ-opioidergic cell types.Nature communications · 2023Article
- Chemical tools for the opioids.Molecular and cellular neurosciences · 2023Review
- Emerging approaches for decoding neuropeptide transmission.Trends in neurosciences · 2022Review
- Caged-carvedilol as a new tool for visible-light photopharmacology of β-adrenoceptors in native tissues.iScience · 2022Article
- The emergence of molecular systems neuroscience.Molecular brain · 2022Review
- Structure-based development of caged dopamine DScientific reports · 2020Article
- Optogenetic Techniques for Manipulating and Sensing G Protein-Coupled Receptor Signaling.Methods in molecular biology (Clifton, N.J.) · 2020Review
- Article
- Optical control of neuronal ion channels and receptors.Nature reviews. Neuroscience · 2019Review
- A Caged Enkephalin Optimized for Simultaneously Probing Mu and Delta Opioid Receptors.ACS chemical neuroscience · 2018Article
- Article
- Optogenetic approaches for dissecting neuromodulation and GPCR signaling in neural circuits.Current opinion in pharmacology · 2017Review
- New Technologies for Elucidating Opioid Receptor Function.Trends in pharmacological sciences · 2016Review
- The μ-opioid receptor: an electrophysiologist's perspective from the sharp end.British journal of pharmacology · 2015Review
- Desensitization of functional µ-opioid receptors increases agonist off-rate.Molecular pharmacology · 2014Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
The spatiotemporal dynamics of opioid signaling in the brain remain poorly defined. Photoactivatable opioid ligands provide a means to quantitatively measure these dynamics and their underlying mechanisms in brain tissue. Although activation kinetics can be assessed using caged agonists, deactivation kinetics are obscured by slow clearance of agonist in tissue. To reveal deactivation kinetics of opioid signaling we developed a caged competitive antagonist that can be quickly photoreleased in sufficient concentrations to render agonist dissociation effectively irreversible. Carboxynitroveratryl-naloxone (CNV-NLX), a caged analog of the competitive opioid antagonist NLX, was readily synthesized from commercially available NLX in good yield and found to be devoid of antagonist activity at heterologously expressed opioid receptors. Photolysis in slices of rat locus coeruleus produced a rapid inhibition of the ionic currents evoked by multiple agonists of the μ-opioid receptor (MOR), but not of α-adrenergic receptors, which activate the same pool of ion channels. Using the high-affinity peptide agonist dermorphin, we established conditions under which light-driven deactivation rates are independent of agonist concentration and thus intrinsic to the agonist-receptor complex. Under these conditions, some MOR agonists yielded deactivation rates that are limited by G protein signaling, whereas others appeared limited by agonist dissociation. Therefore, the choice of agonist determines which feature of receptor signaling is unmasked by CNV-NLX photolysis.
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.