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Showing 1-30 of 107 results for "U4133" within Papers
Marek Zubrzycki et al.
British journal of pharmacology, 174(21), 3780-3789 (2017-08-05)
Endocannabinoids and opioids play a vital role in mediating pain-induced analgesia. The specific effects of these compounds within the orofacial region are largely unknown. In this study, we tried to determine whether an increase in cannabinoid and opioid concentration in
Simon Nicolussi et al.
Biochemical pharmacology, 92(4), 669-689 (2014-10-07)
Besides the suggested role of a putative endocannabinoid membrane transporter mediating the cellular uptake of the endocannabinoid anandamide (AEA), this process is intrinsically coupled to AEA degradation by the fatty acid amide hydrolase (FAAH). Differential blockage of each mechanism is
Janani Ravi et al.
Oncotarget, 5(9), 2475-2486 (2014-05-09)
The endocannabinoid anandamide (AEA), a neurotransmitter was shown to have anti-cancer effects. Fatty acid amide hydrolase (FAAH) metabolizes AEA and decreases its anti-tumorigenic activity. In this study, we have analyzed the role of FAAH inhibition in non-small cell lung cancer
Florian M Dato et al.
Analytical biochemistry, 546, 50-57 (2018-02-07)
Fatty acid amide hydrolase (FAAH) is involved in many human diseases, particularly cancer, pain and inflammation as well as neurological, metabolic and cardiovascular disorders. Therefore, FAAH is an attractive target for the development of low-molecular-weight inhibitors as therapeutics, which requires
Lindsey N Friend et al.
Molecules (Basel, Switzerland), 24(7) (2019-04-17)
The hippocampus is thought to encode information by altering synaptic strength via synaptic plasticity. Some forms of synaptic plasticity are induced by lipid-based endocannabinoid signaling molecules that act on cannabinoid receptors (CB1). Endocannabinoids modulate synaptic plasticity of hippocampal pyramidal cells
Mireille Alhouayek et al.
Scientific reports, 10(1), 6314-6314 (2020-04-15)
There is good evidence that the N-acylethanolamine (NAE)/monoacylglycerol (MAG) signalling systems are involved in the pathogenesis of cancer. However, it is not known how prostate tumours affect these systems in the surrounding non-malignant tissue and vice versa. In the present
Wende Niforatos et al.
Molecular pharmacology, 71(5), 1209-1216 (2007-02-23)
As a member of the transient receptor potential (TRP) ion channel superfamily, the ligand-gated ion channel TRPA1 has been implicated in nociceptive function and pain states. The endogenous ligands that activate TRPA1 remain unknown. However, various agonists have been identified
Amaia M Erdozain et al.
Addiction biology, 20(4), 773-783 (2014-07-22)
There is strong biochemical, pharmacological and genetic evidence for the involvement of the endocannabinoid system (ECS) in alcohol dependence. However, the majority of studies have been performed in animal models. The aim of the present study was to assess the
Armando Silva-Cruz et al.
Frontiers in pharmacology, 8, 921-921 (2018-01-10)
Cannabinoid receptor 1 (CB
Joseph K Ritter et al.
The Journal of pharmacology and experimental therapeutics, 376(1), 1-11 (2020-10-23)
The endocannabinoid, anandamide (AEA), stimulates cannabinoid receptors (CBRs) and is enriched in the kidney, especially the renal medulla. AEA infused into the renal outer medulla of mice stimulates urine flow rate and salt excretion. Here we show that these effects
Kazuma Sekiba et al.
Scientific reports, 10(1), 15556-15556 (2020-09-25)
MICA/B proteins are expressed on the surface of various types of stressed cells, including cancer cells. Cytotoxic lymphocytes expressing natural killer group 2D (NKG2D) receptor recognize MICA/B and eliminate the cells. However, cancer cells evade such immune recognition by inducing
The FAAH inhibitor URB597 suppresses hippocampal maximal dentate afterdischarges and restores seizure-induced impairment of short and long-term synaptic plasticity
Colangeli R, et al.
Scientific Reports, 7(1), 11152-11152 (2017)
Interaction between the cholecystokinin and endogenous cannabinoid systems in cued fear expression and extinction retention
Bowers ME and Ressler KJ
Neuropsychopharmacology, 30, 688-688 (2015)
Mechanism of carbamate inactivation of FAAH: implications for the design of covalent inhibitors and in vivo functional probes for enzymes
Alexander JP and Cravatt BF
Chemistry & Biology, 12(11), 1179-1187 (2005)
A A Martinez et al.
Neurobiology of disease, 74, 295-304 (2014-12-09)
Long-term administration of l-3,4-dihydroxyphenylalanine (levodopa), the mainstay treatment for Parkinson's disease (PD), is accompanied by fluctuations in its duration of action and motor complications (dyskinesia) that dramatically affect the quality of life of patients. Levodopa-induced dyskinesias (LID) can be modeled
Stefania Petrosino et al.
The Journal of pharmacology and experimental therapeutics, 365(3), 652-663 (2018-04-11)
Phytocannabinoids modulate inflammatory responses by regulating the production of cytokines in several experimental models of inflammation. Cannabinoid type-2 (CB2) receptor activation was shown to reduce the production of the monocyte chemotactic protein-2 (MCP-2) chemokine in polyinosinic-polycytidylic acid [poly-(I:C)]-stimulated human keratinocyte
Zoltan Balogh et al.
Progress in neuro-psychopharmacology & biological psychiatry, 90, 84-91 (2018-11-21)
Endocannabinoids (eCBs) anandamide (AEA) and 2-arachidonoylglycerol (2-AG) were shown to be involved in the basis of trauma-induced behavioral changes, particularly contextual conditioned fear, however, their ligand-specific effects and possible interactions are poorly understood. Here we assessed specific eCB effects and
Xing-Qin Wang et al.
British journal of pharmacology, 173(7), 1143-1153 (2014-10-10)
The endocannabinoid (eCB) system is involved in pathways that regulate drug addiction and eCB-mediated synaptic plasticity has been linked with addictive behaviours. Here, we investigated the molecular mechanisms underlying the changes in eCB-dependent synaptic plasticity in the nucleus accumbens core
Michał Biernacki et al.
Molecules (Basel, Switzerland), 23(9) (2018-09-19)
Fatty acid amide hydrolase (FAAH) inhibitor [3-(3-carbamoylphenyl)phenyl] N-cyclohexylcarbamate (URB597) may influence redox balance and blood pressure through the modulation of endocannabinoids levels. Therefore, this study aimed to compare changes in oxidative metabolism and apoptosis in the hearts of rats with
Cannabinoids Activate Monoaminergic Signaling to Modulate Key
Mitchell D Oakes et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 37(11), 2859-2869 (2017-02-12)
Luara A Batista et al.
Behavioural brain research, 317, 508-514 (2016-10-28)
Selective stimulation of carotid chemoreceptors by intravenous infusion of low doses of potassium cyanide (KCN) produces short-lasting escape responses that have been proposed as a model of panic attack. In turn, preclinical studies suggest that facilitation of the endocannabinoid system
Iryna A Khasabova et al.
Pharmacological research, 90, 67-75 (2014-10-12)
Cisplatin has been used effectively to treat a variety of cancers but its use is limited by the development of painful peripheral neuropathy. Because the endocannabinoid 2-arachidonoyl-sn-glycerol (2-AG) is anti-hyperalgesic in several preclinical models of chronic pain, the anti-hyperalgesic effect
Karl Kevala et al.
International journal of molecular sciences, 21(22) (2020-11-26)
We investigated the synthesis of N-docosahexaenoylethanolamine (synaptamide) in neuronal cells from unesterified docosahexaenoic acid (DHA) or DHA-lysophosphatidylcholine (DHA-lysoPC), the two major lipid forms that deliver DHA to the brain, in order to understand the formation of this neurotrophic and neuroprotective
Verginia C Cuzon Carlson et al.
Nature communications, 11(1), 2555-2555 (2020-05-24)
Fetal alcohol exposure (FAE) is the leading preventable developmental cause of cognitive dysfunction. Even in the absence of binge drinking, alcohol consumption during pregnancy can leave offspring deficient. However, the mechanisms underlying these deficiencies are unknown. Using a mouse model
Nurcan Calimli Tosun et al.
Journal of neural transmission (Vienna, Austria : 1996), 122(3), 363-367 (2014-06-12)
Itch and pain are two irritating sensations sharing a lot in common. Considering the antinociceptive effects of blockade of endocannabinoid degrading enzymes in pain states, we attempted to reduce scratching behavior by endocannabinoid modulation, i.e. by inhibiting fatty acid amide
Romain Dalmann et al.
Neuropharmacology, 91, 63-70 (2014-12-03)
Paracetamol (acetaminophen) is the most commonly used analgesic in the world. Recently, a new view of its action has emerged: that paracetamol would be a pro-drug that should be metabolized by the FAAH enzyme into AM404, its active metabolite. However
Martin A Sticht et al.
Neuropharmacology, 102, 92-102 (2015-11-07)
Cannabinoid (CB) agonists suppress nausea in humans and animal models; yet, their underlying neural substrates remain largely unknown. Evidence suggests that the visceral insular cortex (VIC) plays a critical role in nausea. Given the expression of CB1 receptors and the
Sally Miller et al.
Experimental eye research, 201, 108266-108266 (2020-09-27)
Cannabinoids are part of an endogenous signaling system found throughout the body, including the eye. Hepler and Frank showed in the early 1970s that plant cannabinoids can lower intraocular pressure (IOP), an effect since shown to occur via cannabinoid CB1
Olga A Sergeeva et al.
Neuropharmacology, 119, 111-122 (2017-04-13)
N-oleoyl-dopamine (OLDA) is an amide of dopamine and oleic acid, synthesized in catecholaminergic neurons. The present study investigates OLDA targets in midbrain dopaminergic (DA) neurons. Substantia Nigra compacta (SNc) DA neurons recorded in brain slices were excited by OLDA in
Milica Jankovic et al.
Physiology & behavior, 227, 113174-113174 (2020-09-24)
Sex differences in the susceptibility to chronic unpredictable stress (CUS) and the effects of fatty acid amide hydrolase (FAAH) inhibitor URB597 in rats have been investigated in this study. In this context, we investigated the effects of prolonged treatment with
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