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Longhe Yang, Long Li, Ling Chen, Yanting Li, Huixia Chen, Yuhang Li, Guangnian Ji, Donghai Lin, Zuguo Liu, Yan Qiu
Pharmacological blockade of N-acylethanolamine acid amidase (NAAA) activity is an available approach for inflammation and pain control through restoring the ability of endogenous PEA. But the recently reported NAAA inhibitors suffer from the chemical and biological unstable properties, which restrict functions of NAAA inhibition in vivo. It is still unrevealed whether systematic inhibition of NAAA could modulate PEA-mediated pain signalings. Here we reported an oxazolidinone imide compound 3-(6-phenylhexanoyl) oxazolidin-2-one (F96), which potently and selectively inhibited NAAA activity (IC50 = 270 nM)...
2015: Scientific Reports
Ferge Zsigmond
On 10th of July 2014 the European Court of Justice made in his decisions in relation to the cases D. (C-358/13) and G. (C-181/14) an interpretation, that the concept of 'medicinal product' according to the law of the European Union does not include the materials, which are - as not covering substances, such as those at issue in the main proceedings, which produce effects that merely modify physiological functions but which are not such as to have any beneficial effects, either immediately or in the long term, on human health, are consumed solely to induce a state of intoxication and are, as such, harmful to human health...
November 30, 2014: Orvosi Hetilap
N I Levchuk
It is known from literature about antioxidant, anti-inflammatory, membrane protective and adreniregulatory properties of N-acetylethanolamines, but data concerning their participation in regulation of steroidogenesis are insufficient. In order to study the influence of a synthetic analogue of endogenous canabinoid anandamide - metanandamide - on the intensity of steroidogenesis the influence of different concentrations of the drug on the contents of 11-hydroxicorticosteroides (11-HCS) in the culture medium after incubation of adrenal tissue in rats of both sexes was investigated...
July 2013: Ukraïnsʹkyĭ Biokhimichnyĭ Z︠h︡urnal
Randa L Stringer, Benjamin I Laufer, Morgan L Kleiber, Shiva M Singh
BACKGROUND: Prenatal alcohol exposure is known to result in fetal alcohol spectrum disorders, a continuum of physiological, behavioural, and cognitive phenotypes that include increased risk for anxiety and learning-associated disorders. Prenatal alcohol exposure results in life-long disorders that may manifest in part through the induction of long-term gene expression changes, potentially maintained through epigenetic mechanisms. FINDINGS: Here we report a decrease in the expression of Canabinoid receptor 1 (Cnr1) and an increase in the expression of the regulatory microRNA miR-26b in the brains of adult mice exposed to ethanol during neurodevelopment...
2013: Clinical Epigenetics
Jacob N Ablin, Dan Buskila
Fibromyalgia is a syndrome characterized by the presence of chronic widespread pain, representing sensitization of the central nervous system. The pthophysiology of fibromyalgia is a complex and remains in evolution, encompassing diverse issues such as disturbed patterns of sleep, alter processing and decreased conditioned pain modulation at the spinal level, as well as increased connectivity between various pain - processing areas of the brain. This evolution is continuously uncovering potential novel therapeutic targets...
August 2013: Maturitas
Morgan Le Naour, Eyup Akgün, Ajay Yekkirala, Mary M Lunzer, Mike D Powers, Alexander E Kalyuzhny, Philip S Portoghese
Given that μ opioid (MOP) and canabinoid (CB1) receptors are colocalized in various regions of the central nervous system and have been reported to associate as heteromer (MOP-CB1) in cultured cells, the possibility of functional, endogenous MOP-CB1 in nociception and other pharmacologic effects has been raised. As a first step in investigating this possibility, we have synthesized a series of bivalent ligands 1-5 that contain both μ agonist and CB1 antagonist pharmacophores for use as tools to study the functional interaction between MOP and CB1 receptors in vivo...
July 11, 2013: Journal of Medicinal Chemistry
Ki-Yeol Yoo, So-Young Park
Alzheimer's disease (AD) is one of the most well-known neurodegenerative diseases and explains 50-60% of dementia in patients. The prevalence rate of AD is positively correlated with age and AD affects ≥ 40% of those over 85 years old. The major AD therapeutics available on the market are acetylcholinesterase inhibitors, such as tacrine and donepezil. New therapeutic agents that can block the disease-inducing mechanisms are essential. Diverse efforts have been made to discover anti-AD agents from natural sources...
2012: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Kanwaljit Chopra, Anurag Kuhad, Vipin Arora
INTRODUCTION: Fibromyalgia is a debilitating, chronic pain disorder typically present with allodynia and hyperalgesia. Estimates from the USA suggest that fibromyalgia affects about 5% of women, and is the third most common rheumatic disorder after lower back pain and osteoarthritis. Recent research advances highlighted a role for aberrant central pain processing in fibromyalgia, and consistent with this, the first three drugs (pregabalin, duloxetine and milnacipran) approved by the FDA for fibromyalgia over the past 2 years have a predominantly central mode of action...
November 2011: Expert Opinion on Therapeutic Targets
María L López-Rodríguez, Alma Viso, Silvia Ortega-Gutiérrez, Inés Díaz-Laviada
The endogenous canabinoid system (ECS) is involved in the regulation of an important number of central and peripheral physiological effects. Among all these functions, the control of the cellular proliferation has become a focus of major attention as opening new therapeutic possibilities for the use of cannabinoids as potential antitumor agents. The capacity of endogenous and synthetic cannabinoids to induce apoptosis of different tumoral cells in culture and in vivo, the mechanism underlying and the potential therapeutic applications are discussed in this review...
January 2005: Mini Reviews in Medicinal Chemistry
R Boskovic, J Klein, C Woodland, T Karaskov, G Koren
There is wide variability in the reported adverse fetal effects of cocaine and cannabinoids. The causes of this variability are largely unknown. We hypothesized that variability in placental handling of drugs affect fetal exposure. We used twin pregnancies as a paradigm to address the role of the placenta in this variability. We analyzed hair or meconium samples taken from dizygotic and monozygotic twins exposed in utero to illicit drugs. Out of 12 pairs, 5 had negative levels in both twins, and seven pairs of twins had chemical evidence of fetal exposure to cocaine (n = 5) or cannabinoids (n = 2)...
November 2001: Canadian Journal of Physiology and Pharmacology
M Beltramo, E di Tomaso, D Piomelli
Anandamide, an endogenous canabinoid substance, is hydrolyzed by an amidohydrolase activity present in rat brain and liver. We report that the bromoenol lactone, (E)-6-(bromomethylene) tetrahydro-3-(1-naphthalenyl)-2H-pyran-2-one (BTNP), is a potent inhibitor of this enzyme activity. BTNP prevented anandamide hydrolysis in rat brain microsomes with an IC50 of 0.8 +/- 0.3 microM. Kinetic and dialysis experiments indicated that this effect was non-competitive and irreversible. After chromatographic fractionation of the enzyme activity, BTNP was still effective, suggesting that it interacts directly with the enzyme...
February 24, 1997: FEBS Letters
W Van der Kloot
Anandamide (arachydonylethanolamide) is a naturally-occurring ligand of the canabinoid receptor. When anandamide binds to its receptor, adenylate cyclase is inhibited. At the frog neuromuscular junction, anandamide lessened the increase in quantal size produced by pretreatment in hypertonic solution. It did not alter the increases in quantal size produced by insulin or by a permeable agonist of cAMP. It was known that hypertonic treatment increases quantal size by way of the cAMP-protein kinase A pathway. Anandamide had no effect on miniature endplate potential frequency (fmepp) in untreated preparations...
June 27, 1994: Brain Research
J Gallardo, M Fodor
Nausea and vomiting are a serious side effect of chemotherapy, frequently leading to failure of treatment compliance. Chemotherapeutic agents act preferentially on the chemo-receptor trigger zone located at the floor of the 4th ventricle. Vomiting may develop at initiation of therapy or several days later. Phenotiazine derivatives, butyrophenones or methochlopramide are particularly useful by their anti-dopaminergic effects. Canabinoids or steroids may be also useful. Combinations of drugs are frequently required...
November 1989: Revista Médica de Chile
R Mechoulam, W A Devane, A Breuer, J Zahalka
The present overview covers various aspects of research going on in the Cannabis field in the Department of Natural Products at the Hebrew University. In the first part we discuss, and try to explain, the reason for the absence of the term Cannabis (and possibly also opium) in the Old Testament. In the second part we bring evidence that, contrary to widely held views, stereospecificity of cannabinoid action is extremely high, and in certain cases almost absolute. Previous results seem to have been due to impurities in the samples tested...
November 1991: Pharmacology, Biochemistry, and Behavior
G Koren, K Graham
During the last decades there has been a substantial increase in the recreational use of cocaine in young adults and parallelly there has been an increase of its use by pregnant women. We analyzed all published papers on cocaine use in pregnancy and found that for most endpoints studied (eg, prematurity, head circumference) there were many studies showing effects and many showing no effects. Upon meta-analysis, most of these effects could not be shown significant when compared to control groups. In a prospective study in Toronto, babies exposed to cocaine during the first trimester only had Bayley scores at 18-mo of life that were identical to unexposed babies or to those exposed to canabinoids...
June 1992: Veterinary and Human Toxicology
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