Search Results - "GRAZIA CASCIO, Maria"
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Characterization of cannabinoid receptor ligands in tissues natively expressing cannabinoid CB2 receptors
Published in British journal of pharmacology (01-06-2013)“…Background and Purpose Although cannabinoid CB2 receptor ligands have been widely characterized in recombinant systems in vitro, little pharmacological…”
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2
Gradient of 2-Arachidonoylglycerol Regulates Mouse Epididymal Sperm Cell Start-Up
Published in Biology of reproduction (01-02-2010)“…During transit through the epididymis, spermatozoa are normally kept immotile and do not attain the ability to become motile until they reach the caudal…”
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Changes in endocannabinoid contents in the brain of rats chronically exposed to nicotine, ethanol or cocaine
Published in Brain research (01-11-2002)“…Despite recent data suggesting that the endocannabinoid transmission is a component of the brain reward system and plays a role in dependence/withdrawal to…”
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Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: A critical revisitation
Published in European journal of medicinal chemistry (2008)“…We have synthesized a series of 18 1,5- and 2,5-disubstituted carbamoyl tetrazoles, including LY2183240 ( 1) and LY2318912 ( 7), two compounds previously…”
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5
New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists
Published in Bioorganic & medicinal chemistry letters (01-12-2007)“…A series of new 1,8-naphthyridine and quinoline derivatives were synthesized and evaluated for their cannabinoid receptor affinity. In particular, compounds 2,…”
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6
Novel sterically hindered cannabinoid CB1 receptor ligands
Published in Bioorganic & medicinal chemistry (01-08-2008)“…In the present study, 11 novel N-(3,3-diphenyl)propyl-2,2-diphenylacetamide derivatives (4a-d and 9a-g) and six triphenylacetamides (10a-c and 11a-c) were…”
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A structure–activity relationship study on N-arachidonoyl-amino acids as possible endogenous inhibitors of fatty acid amide hydrolase
Published in Biochemical and biophysical research communications (30-01-2004)“…N-arachidonoyl-glycine (NAGly) has been recently identified in rodent tissues and found to exhibit analgesic activity in vivo. NAGly is a potent inhibitor of…”
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8
Design, synthesis, binding, and molecular modeling studies of new potent ligands of cannabinoid receptors
Published in Bioorganic & medicinal chemistry (15-08-2007)“…In our ongoing program aimed at the design, synthesis, and biological evaluation of novel cannabinoid receptor ligands derived from olivetol and…”
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Cloning of the First sn1-DAG Lipases Points to the Spatial and Temporal Regulation of Endocannabinoid Signaling in the Brain
Published in The Journal of cell biology (10-11-2003)“…Diacylglycerol (DAG) lipase activity is required for axonal growth during development and for retrograde synaptic signaling at mature synapses. This enzyme…”
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10
CB1 Cannabinoid Receptors and On-Demand Defense against Excitotoxicity
Published in Science (American Association for the Advancement of Science) (03-10-2003)“…Abnormally high spiking activity can damage neurons. Signaling systems to protect neurons from the consequences of abnormal discharge activity have been…”
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Investigations on the 4-quinolone-3-carboxylic acid motif. 6. Synthesis and pharmacological evaluation of 7-substituted quinolone-3-carboxamide derivatives as high affinity ligands for cannabinoid receptors
Published in European journal of medicinal chemistry (01-12-2012)“…Within our studies on structure–activity relationships of 4-quinolone-3-carboxamides as cannabinoid ligands, a new series of compounds characterized by a…”
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12
1,2,3-Triazole Ring as a Peptido- and Olefinomimetic Element: Discovery of Click Vanilloids and Cannabinoids
Published in Angewandte Chemie (International ed.) (01-01-2007)“…Fooling nature: The replacement of amide and alkene groups in a biological setting with the 1,2,3‐triazole group led to the discovery of compounds with a…”
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13
New N-Arachidonoylserotonin Analogues with Potential “Dual” Mechanism of Action against Pain
Published in Journal of medicinal chemistry (27-12-2007)“…N-Arachidonoylserotonin (AA-5-HT, 1a) is an inhibitor of fatty acid amide hydrolase (FAAH) that acts also as an antagonist of transient receptor potential…”
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Investigations on the 4-Quinolone-3-carboxylic Acid Motif. 3. Synthesis, Structure−Affinity Relationships, and Pharmacological Characterization of 6-Substituted 4-Quinolone-3-carboxamides as Highly Selective Cannabinoid-2 Receptor Ligands
Published in Journal of medicinal chemistry (26-08-2010)“…A set of quinolone-3-carboxamides 2 bearing diverse substituents at position 1, 3, and 6 of the bicyclic nucleus was prepared. Except for six compounds…”
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15
Rational Design, Synthesis, and Pharmacological Properties of New 1,8-Naphthyridin-2(1H)-on-3-Carboxamide Derivatives as Highly Selective Cannabinoid-2 Receptor Agonists
Published in Journal of medicinal chemistry (25-06-2009)“…The CB2 receptor activation can be exploited for the treatment of diseases such as chronic pain and tumors of immune origin, devoid of psychotropic activity…”
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Development of the first potent and specific inhibitors of endocannabinoid biosynthesis
Published in Biochimica et biophysica acta (01-02-2006)“…Enzymes for the biosynthesis and degradation of the endocannabinoid 2-arachidonoyl glycerol (2-AG) have been cloned and are the sn-1-selective-diacylglycerol…”
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17
Structural and pharmacological analysis of O-2050, a putative neutral cannabinoid CB1 receptor antagonist
Published in European journal of pharmacology (25-01-2011)“…Rimonabant, the prototypic antagonist of cannabinoid CB1 receptors, has been reported to have inverse agonist properties at higher concentrations, which may…”
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Changes in endocannabinoid levels in a rat model of behavioural sensitization to morphine
Published in The European journal of neuroscience (01-10-2004)“…The opioid and cannabinoid systems co‐operate to regulate physiological processes such as nociception and reward. The endocannabinoid system may be a component…”
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New tetrazole-based selective anandamide uptake inhibitors
Published in Bioorganic & medicinal chemistry (01-05-2008)“…A new series of 1,5-and 2,5-disubstituted tetrazoles have been synthesized and evaluated as inhibitors of anandamide cellular uptake. Some of them inhibit the…”
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New Resorcinol−Anandamide “Hybrids” as Potent Cannabinoid Receptor Ligands Endowed with Antinociceptive Activity in Vivo
Published in Journal of medicinal chemistry (23-04-2009)“…Bearing in mind the pharmacophoric requirements of both (−)-trans-Δ9-tetrahydrocannabinol (THC) and anandamide (AEA), we designed a novel pharmacophore…”
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