Literature DB >> 19266526

Synthesis and pharmacological activity of a potent inhibitor of the biosynthesis of the endocannabinoid 2-arachidonoylglycerol.

Tiziana Bisogno1, James J Burston, Ravi Rai, Marco Allarà, Bijali Saha, Anu Mahadevan, Raj K Razdan, Jenny L Wiley, Vincenzo Di Marzo.   

Abstract

Biosynthesis Inhibition: O-5596, a new inhibitor of the biosynthesis of the endocannabinoid, 2-arachidonoylglycerol, was synthesized and found to be potent (IC(50)=100 nM) and selective versus other proteins and enzymes of the endocannabinoid system in vitro and active in vivo at reducing food intake in mice.

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Year:  2009        PMID： 19266526     DOI： 10.1002/cmdc.200800442

Source DB:  PubMed          Journal:  ChemMedChem        ISSN： 1860-7179            Impact factor:   3.466


  12 in total

1.  Endocannabinoid signaling in the brain: biosynthetic mechanisms in the limelight.

Authors:  Vincenzo Di Marzo
Journal:  Nat Neurosci       Date:  2011-01       Impact factor: 24.884

2.  Assay and inhibition of diacylglycerol lipase activity.

Authors:  Meghan Johnston; Shachi R Bhatt; Surina Sikka; Richard W Mercier; Jay M West; Alexandros Makriyannis; S John Gatley; Richard I Duclos
Journal:  Bioorg Med Chem Lett       Date:  2012-06-06       Impact factor: 2.823

Review 3.  Chemical approaches to therapeutically target the metabolism and signaling of the endocannabinoid 2-AG and eicosanoids.

Authors:  Rebecca A Kohnz; Daniel K Nomura
Journal:  Chem Soc Rev       Date:  2014-03-28       Impact factor: 54.564

4.  Inhibiting endocannabinoid biosynthesis: a novel approach to the treatment of constipation.

Authors:  M Bashashati; Y Nasser; C M Keenan; W Ho; F Piscitelli; M Nalli; K Mackie; M A Storr; V Di Marzo; K A Sharkey
Journal:  Br J Pharmacol       Date:  2015-04-23       Impact factor: 8.739

Review 5.  New horizons on the role of cannabinoid CB1 receptors in palatable food intake, obesity and related dysmetabolism.

Authors:  L Cristino; L Palomba; V Di Marzo
Journal:  Int J Obes Suppl       Date:  2014-07-08

6.  Effects of cannabinoids and cannabinoid-enriched Cannabis extracts on TRP channels and endocannabinoid metabolic enzymes.

Authors:  Luciano De Petrocellis; Alessia Ligresti; Aniello Schiano Moriello; Marco Allarà; Tiziana Bisogno; Stefania Petrosino; Colin G Stott; Vincenzo Di Marzo
Journal:  Br J Pharmacol       Date:  2011-08       Impact factor: 8.739

7.  An inverse agonist of estrogen-related receptor γ regulates 2-arachidonoylglycerol synthesis by modulating diacylglycerol lipase expression in alcohol-intoxicated mice.

Authors:  Yoon Seok Jung; Yong-Hoon Kim; Kamalakannan Radhakrishnan; Jina Kim; Don-Kyu Kim; Ji-Hyeok Lee; Hyunhee Oh; In-Kyu Lee; Wook Kim; Sung Jin Cho; Cheol Soo Choi; Steven Dooley; Josephine M Egan; Chul-Ho Lee; Hueng-Sik Choi
Journal:  Arch Toxicol       Date:  2020-01-07       Impact factor: 5.153

8.  A novel fluorophosphonate inhibitor of the biosynthesis of the endocannabinoid 2-arachidonoylglycerol with potential anti-obesity effects.

Authors:  Tiziana Bisogno; Anu Mahadevan; Roberto Coccurello; Jae Won Chang; Marco Allarà; Yugang Chen; Giacomo Giacovazzo; Aron Lichtman; Benjamin Cravatt; Anna Moles; Vincenzo Di Marzo
Journal:  Br J Pharmacol       Date:  2013-06       Impact factor: 8.739

Review 9.  Endocannabinoids--at the crossroads between the gut microbiota and host metabolism.

Authors:  Patrice D Cani; Hubert Plovier; Matthias Van Hul; Lucie Geurts; Nathalie M Delzenne; Céline Druart; Amandine Everard
Journal:  Nat Rev Endocrinol       Date:  2015-12-18       Impact factor: 43.330

10.  Complementary synaptic distribution of enzymes responsible for synthesis and inactivation of the endocannabinoid 2-arachidonoylglycerol in the human hippocampus.

Authors:  A Ludányi; S S-J Hu; M Yamazaki; A Tanimura; D Piomelli; M Watanabe; M Kano; K Sakimura; Z Maglóczky; K Mackie; T F Freund; I Katona
Journal:  Neuroscience       Date:  2010-10-28       Impact factor: 3.590
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