Methods of treating mental diseases, inflammation and pain
作者： Daniele Piomelli , Massimiliano Beltramo
DOI:
关键词: Chemistry 、 Anandamide amidohydrolase 、 Aryl 、 Inflammation 、 Stereochemistry 、 Lactone
摘要: Methods are disclosed for treating or preventing disorders such as mental diseases, inflammation and pain by inhibiting the enzyme anandamide amidohydrolase. A therapeutically effective level of an amidohydrolase inhibitor is administered a haloenol lactone. Preferably, lactone formula (I) wherein R hydrogen, R1 halogen, R2 selected from group consisting aryl, aryloxy, heteroaryl radicals, derivatives said lactones, mixtures thereof. The lactone, E-6-(bromomethylene)tetrahydro-3-(1-naphthalenyl)-2H-pyrane-2-one, most preferred.
lens.org 参考文章(15)
Alexander Krantz, Tim F. Tam, Robin W. Spencer, Ynenolactone protease inhibitors ,(1984)
Randy H. Weiss, Method of selectively inhibiting calcium-independent myocardial phospholipase A2 ,(1990)
S L Hazen, L A Zupan, R H Weiss, D P Getman, R W Gross, Suicide inhibition of canine myocardial cytosolic calcium-independent phospholipase A2. Mechanism-based discrimination between calcium-dependent and -independent phospholipases A2. Journal of Biological Chemistry. ,vol. 266, pp. 7227- 7232 ,(1991) , 10.1016/S0021-9258(20)89634-3
Kurt Kesseler, Gunther Wess, Gerhard Beck, Heiner Jendralla, 4-hydroxytetrahydropyran-2-ones and the corresponding dihydroxycarboxylic acid derivatives, salts and esters and a process for their preparation ,(1990)
Franck Desarnaud, Hugues Cadas, Daniele Piomelli, Anandamide Amidohydrolase Activity in Rat Brain Microsomes Journal of Biological Chemistry. ,vol. 270, pp. 6030- 6035 ,(1995) , 10.1074/JBC.270.11.6030
Christopher Norman Lewis, Jonathan Philip Dickens, Christopher David Floyd, Alan Hornsby Davidson, 6-(hydronaphtyl-1-ethyl)-4-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-ones and the corresponding hydroxy acids ,(1990)
Floyd H. Chilton, James Scott Dixon, Ruth Judik Mayer, Ralph Floyd Hall, James David Winkler, Lisa Ann Marshall, Anti-inflammatory compounds ,(1995)
P. E. Mallet, R. J. Beninger, The endogenous cannabinoid receptor agonist anandamide impairs memory in rats Behavioural Pharmacology. ,vol. 7, pp. 276- 284 ,(1996) , 10.1097/00008877-199605000-00008
J. Balsinde, I. D. Bianco, E. J. Ackermann, K. Conde-Frieboes, E. A. Dennis, Inhibition of calcium-independent phospholipase A2 prevents arachidonic acid incorporation and phospholipid remodeling in P388D1 macrophages. Proceedings of the National Academy of Sciences. ,vol. 92, pp. 8527- 8531 ,(1995) , 10.1073/PNAS.92.18.8527
A. Fontana, V. Di Marzo, H. Cadas, D. Piomelli, Analysis of anandamide, an endogenous cannabinoid substance, and of other natural N-acylethanolamines Prostaglandins Leukotrienes and Essential Fatty Acids. ,vol. 53, pp. 301- 308 ,(1995) , 10.1016/0952-3278(95)90130-2