5 research outputs found
New metabolically stable fatty acid amide ligands of cannabinoid receptors: synthesis and receptor affinity studies
Get PDFWe investigated the structure-activity relationships for the interactions of fatty acid amide analogs of the endocannabinoid anandamide with human recombinant cannabinoid receptors. Thirty-five novel fatty acid amides were synthesized using five different types of acyl chains and 11 different aromatic amine 'heads.' Although none of the new compounds was a more potent ligand than anandamide, we identified three amine groups capable of improving the metabolic stability of arachidonoylamides and their CBI/CB2 selectivity ratio to over 20-fold, and several aromatic amines capable of improving the affinity of short chain or monosaturated fatty acids for cannabinoid CBI receptors. For the first time a tertiary amide of arachidonic acid was found to possess moderate affinity (K, = 300 nM) for cannabinoid CBI, but not CB2, receptors
proteomic analysis of the interaction between Brassica napus cv. surpass 400 and virulent or avirulent isolates of Leptosphaeria maculans
No full textOccurence, viability and genotyping of Cryptosporidium and Giardia in influent water and harvested shellfish in the Varano Lagoon (Italy)
No full textCryptosporidium and Giardia in treatment municipal wastwater and water courses flowing into the Varano Logoon (Italy) and in shellfish harvested in the same envinronment.
No full textNew metabolically stable fatty acid amide ligands of cannabinoid receptors: synthesis and receptor affinity studies
No full textWe investigated the structure-activity relationships for the interactions of fatty acid amide analogs of the endocannabinoid anandamide with human recombinant cannabinoid receptors. Thirty-five novel fatty acid amides were synthesized using five different types of acyl chains and 11 different aromatic amine 'heads.' Although none of the new compounds was a more potent ligand than anandamide, we identified three amine groups capable of improving the metabolic stability of arachidonoylamides and their CBI/CB2 selectivity ratio to over 20-fold, and several aromatic amines capable of improving the affinity of short chain or monosaturated fatty acids for cannabinoid CBI receptors. For the first time a tertiary amide of arachidonic acid was found to possess moderate affinity (K, = 300 nM) for cannabinoid CBI, but not CB2, receptors
