ArticleChemistry & biology2010
Inhibitor of fatty acid amide hydrolase normalizes cardiovascular function in hypertension without adverse metabolic effects.
Article in Chemistry & biology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 47 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.
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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
47 citing papers in PubMed, 94 citations in OpenAlex.
- Short Communication: The Peripheral Cannabinoid CBInternational journal of molecular sciences · 2026Article
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- Cardiovascular Effects of Cannabidiol: From Molecular Mechanisms to Clinical Implementation.International journal of molecular sciences · 2025Review
- The relationship between cannabis and cardiovascular disease: clearing the haze.Nature reviews. Cardiology · 2025Review
- Pharmacology of Non-Psychoactive Phytocannabinoids and Their Potential for Treatment of Cardiometabolic Disease.Handbook of experimental pharmacology · 2025Review
- Comprehensive mini-review: therapeutic potential of cannabigerol - focus on the cardiovascular system.Frontiers in pharmacology · 2025Review
- Function of Presynaptic Inhibitory Cannabinoid CBInternational journal of molecular sciences · 2024Article
- Weak Hypotensive Effect of Chronic Administration of the Dual FAAH/MAGL Inhibitor JZL195 in Spontaneously Hypertensive Rats as Revealed by Area under the Curve Analysis.International journal of molecular sciences · 2023Article
- SAR study on Novel truxillic acid monoester-Based inhibitors of fatty acid binding proteins as Next-Generation antinociceptive agents.Bioorganic chemistry · 2022Article
- Fatty acid amide hydrolase activity in the dorsal periaqueductal gray attenuates neuropathic pain and associated dysautonomia.American journal of physiology. Regulatory, integrative and comparative physiology · 2022Article
- Endocannabinoid System in Polycystic Kidney Disease.American journal of nephrology · 2022Article
- Review
- Endocannabinoid System and Its Regulation by Polyunsaturated Fatty Acids and Full Spectrum Hemp Oils.International journal of molecular sciences · 2021Review
- Beneficial Changes in Rat Vascular Endocannabinoid System in Primary Hypertension and under Treatment with Chronic Inhibition of Fatty Acid Amide Hydrolase by URB597.International journal of molecular sciences · 2021Article
- Strategies for Tuning the Selectivity of Chemical Probes that Target Serine Hydrolases.Cell chemical biology · 2020Review
- The FAAH Inhibitor URB597 Modulates Lipid Mediators in the Brain of Rats with Spontaneous Hypertension.Biomolecules · 2020Article
- Experimental Activation of Endocannabinoid System Reveals Antilipotoxic Effects on Cardiac Myocytes.Molecules (Basel, Switzerland) · 2020Article
- Cannabinoid Antagonist Drug Discrimination in Nonhuman Primates.The Journal of pharmacology and experimental therapeutics · 2020Article
- Article
- Cannabinoids in arterial, pulmonary and portal hypertension - mechanisms of action and potential therapeutic significance.British journal of pharmacology · 2019Review
Corrections and comments
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Authors and funding
16 authors at 4 institutions in 1 country.
Funding
Abstract
The enzyme fatty acid amide hydrolase (FAAH) catalyzes the in vivo degradation of the endocannabinoid anandamide, thus controlling its action at receptors. A novel FAAH inhibitor, AM3506, normalizes the elevated blood pressure and cardiac contractility of spontaneously hypertensive rats (SHR) without affecting these parameters in normotensive rats. These effects are due to blockade of FAAH and a corresponding rise in brain anandamide levels, resulting in CB₁ receptor-mediated decrease in sympathetic tone. The supersensitivity of SHR to CB₁ receptor-mediated cardiovascular depression is related to increased G protein coupling of CB₁ receptors. Importantly, AM3506 does not elicit hyperglycemia and insulin resistance seen with other FAAH inhibitors or in FAAH⁻/⁻ mice, which is related to its inability to inhibit FAAH in the liver due to rapid hepatic uptake and metabolism. This unique activity profile offers improved therapeutic value in hypertension.
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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.