ArticleACS medicinal chemistry letters2016
Discovery of KLS-13019, a Cannabidiol-Derived Neuroprotective Agent, with Improved Potency, Safety, and Permeability.
Article in ACS medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
24 citing papers in PubMed, 51 citations in OpenAlex.
- Unveiling the Origin of Regioselectivity in Iron(III)-Promoted Friedel-Crafts Synthesis of Cannabinoids: Theoretical Studies and Synthetic Applications.The Journal of organic chemistry · 2026Article
- Cannabidiol-Based Thiosemicarbazones: A Preliminary Study Evaluating Their Anti-Tyrosinase Properties.Molecules (Basel, Switzerland) · 2025Article
- A concise enzyme cascade enables the manufacture of natural and halogenated protoberberine alkaloids.Nature communications · 2025Article
- KLS-13019, a Novel Structural Analogue of Cannabidiol and GPR55 Receptor Antagonist, Prevents and Reverses Chemotherapy-Induced Peripheral Neuropathy in Rats.The Journal of pharmacology and experimental therapeutics · 2024Article
- Design, Synthesis, and Characterization of Novel Cannabidiol-Based Derivatives with Potent Antioxidant Activities.International journal of molecular sciences · 2024Article
- Knockdown siRNA Targeting GPR55 Reveals Significant Differences Between the Anti-inflammatory Actions of KLS-13019 and Cannabidiol.Journal of molecular neuroscience : MN · 2024Article
- Design, synthesis and antifungal activity of novel amide derivatives containing a pyrrolidine moiety as potential succinate dehydrogenase inhibitors.Molecular diversity · 2024Article
- Knockdown siRNA targeting GPR55 reveals significant differences between the anti-inflammatory actions of KLS-13019 and cannabidiol.Research square · 2024Article
- A critical assessment of the abuse, dependence and associated safety risks of naturally occurring and synthetic cannabinoids.Frontiers in psychiatry · 2024Review
- Unraveling the Neuroprotective Effect of Natural Bioactive Compounds Involved in the Modulation of Ischemic Stroke by Network Pharmacology.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Synthetic Pathways to Non-Psychotropic Phytocannabinoids as Promising Molecules to Develop Novel Antibiotics: A Review.Pharmaceutics · 2023Review
- Efficient Syntheses of KLS-13019 Using Palladium Mediated Cross Couplings.Tetrahedron letters · 2023Article
- Anti-Inflammatory Properties of KLS-13019: a Novel GPR55 Antagonist for Dorsal Root Ganglion and Hippocampal Cultures.Journal of molecular neuroscience : MN · 2022Article
- Curcumin, Resveratrol and Cannabidiol as Natural Key Prototypes in Drug Design for Neuroprotective Agents.Current neuropharmacology · 2022Review
- Using (+)-Carvone to access novel derivatives of (+)-Tetrahedron letters · 2021Article
- Phytocannabinoids: General Aspects and Pharmacological Potential in Neurodegenerative Diseases.Current neuropharmacology · 2021Review
- Neuroprotective Effect of Cannabidiol Against Hydrogen Peroxide in Hippocampal Neuron Culture.Cannabis and cannabinoid research · 2021Article
- Origin of ΔCannabis and cannabinoid research · 2021Article
- The Essential Medicinal Chemistry of Cannabidiol (CBD).Journal of medicinal chemistry · 2020Review
- Article
Corrections and comments
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Authors and funding
11 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Cannabidiol is the nonpsychoactive natural component of C. sativa that has been shown to be neuroprotective in multiple animal models. Our interest is to advance a therapeutic candidate for the orphan indication hepatic encephalopathy (HE). HE is a serious neurological disorder that occurs in patients with cirrhosis or liver failure. Although cannabidiol is effective in models of HE, it has limitations in terms of safety and oral bioavailability. Herein, we describe a series of side chain modified resorcinols that were designed for greater hydrophilicity and "drug likeness", while varying hydrogen bond donors, acceptors, architecture, basicity, neutrality, acidity, and polar surface area within the pendent group. Our primary screen evaluated the ability of the test agents to prevent damage to hippocampal neurons induced by ammonium acetate and ethanol at clinically relevant concentrations. Notably, KLS-13019 was 50-fold more potent and >400-fold safer than cannabidiol and exhibited an in vitro profile consistent with improved oral bioavailability.
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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.