Synthesis and Pharmacological Activity of a Potent Inhibitor of the Biosynthesis of the Endocannabinoid 2-Arachidonoylglycerol

被引：35

作者：

Bisogno, Tiziana ^{[1
]}

Burston, James J. ^{[2
]}

Rai, Ravi ^{[3
]}

Allara, Marco ^{[1
]}

Saha, Bijali ^{[3
]}

Mahadevan, Anu ^{[3
]}

Razdan, Raj K. ^{[3
]}

Wiley, Jenny L. ^{[2
]}

Di Marzo, Vincenzo ^{[1
]}

机构：

[1] CNR, Inst Biomol Chem, Endocannabinoid Res Grp, Pozzuali, NA, Italy

[2] Virginia Commonwealth Univ, Dept Pharmacol & Toxicol, Richmond, VA 23298 USA

[3] Organix Inc, Woburn, MA 01801 USA

来源：

CHEMMEDCHEM | 2009年 / 4卷 / 06期

基金：

美国国家卫生研究院;

关键词：

biosynthesis; CB1; DAGL; endocannabinoids; cannabinoids; receptors; FOOD-INTAKE; SYSTEM;

D O I：

10.1002/cmdc.200800442

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

(Chemical Equation Presented) Biosynthesis Inhibition: O-5596, a new inhibitor of the biosynthesis of the endocannabinoid, 2-arachidonoylglycerol, was synthesized and found to be potent (IC50=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. © 2009 Wiley-VCH Verlag GmbH & Co. KGaA.

引用

页码：946 / 950

页数：5

共 50 条

[31] Genetic Disruption of 2-Arachidonoylglycerol Synthesis Reveals a Key Role for Endocannabinoid Signaling in Anxiety Modulation
Shonesy, Brian C.
Bluett, Rebecca J.
Ramikie, Teniel S.
Baldi, Rita
Hermanson, Daniel J.
Kingsley, Philip J.
Marnett, Lawrence J.
Winder, Danny G.
Colbran, Roger J.
Patel, Sachin
CELL REPORTS, 2014, 9 (05): : 1644 - 1653
[32] Harnessing the Endocannabinoid 2-Arachidonoylglycerol to Lower Intraocular Pressure in a Murine Model
Miller, Sally
Leishman, Emma
Hu, Sherry Shujung
Elghouche, Alhasan
Daily, Laura
Murataeva, Natalia
Bradshaw, Heather
Straiker, Alex
INVESTIGATIVE OPHTHALMOLOGY & VISUAL SCIENCE, 2016, 57 (07) : 3287 - 3296
[33] Genetic Disruption of 2-Arachidonoylglycerol Synthesis Reveals a Key Role for Endocannabinoid Signaling in Anxiety Modulation
Patel, Sachin
Shonesy, Brian
Bluett, Rebecca
Colbran, Roger
Winder, Danny
NEUROPSYCHOPHARMACOLOGY, 2014, 39 : S131 - S131
[34] From Classical to Alternative Pathways of 2-Arachidonoylglycerol Synthesis: AlterAGs at the Crossroad of Endocannabinoid and Lysophospholipid Signaling
Briand-Mesange, Fabienne
Gennero, Isabelle
Salles, Juliette
Trudel, Stephanie
Dahan, Lionel
Ausseil, Jerome
Payrastre, Bernard
Salles, Jean-Pierre
Chap, Hugues
MOLECULES, 2024, 29 (15):
[35] Elevating levels of the endocannabinoid 2-arachidonoylglycerol blunts opioid reward but not analgesia
Martinez-Rivera, Arlene
Fetcho, Robert N.
Birmingham, Lizzie
Xu, Jin
Yang, Ruirong
Foord, Careen
Scala-Chavez, Diego
Mekawy, Narmin
Pleil, Kristen
Pickel, Virginia M.
Liston, Conor
Castorena, Carlos M.
Levitz, Joshua
Pan, Ying-Xian
Briand, Lisa A.
Rajadhyaksha, Anjali M.
Lee, Francis S.
SCIENCE ADVANCES, 2024, 10 (48):
[36] The endocannabinoid 2-arachidonoylglycerol promotes endoplasmic reticulum stress in placental cells
Almada, Marta
Costa, Lia
Fonseca, Bruno
Alves, Patricia
Braga, Jorge
Goncalves, Daniela
Teixeira, Natercia
Correia-da-Silva, Georgina
REPRODUCTION, 2020, 160 (02) : 171 - 180
[37] Endocannabinoid 2-arachidonoylglycerol protects neurons by limiting COX-2 elevation
Zhang, Jian
Chen, Chu
JOURNAL OF BIOLOGICAL CHEMISTRY, 2008, 283 (33) : 22601 - 22611
[38] 2-Arachidonoylglycerol is a substrate for butyrylcholinesterase: A potential mechanism for extracellular endocannabinoid regulation
Barricklow, Jason
Blatnik, Matthew
ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS, 2013, 536 (01) : 1 - 5
[39] The Endocannabinoid 2-arachidonoylglycerol (2-AG) Is Elevated In Acute Ischemic Stroke
Buciuc, Marina
Vasile, Vlad C.
Conte, Gian Marco
Scharf, Eugene
NEUROLOGY, 2020, 94 (15)
[40] Fever Is Mediated by Conversion of Endocannabinoid 2-Arachidonoylglycerol to Prostaglandin E2
Kita, Yoshihiro
Yoshida, Kenij
Tokuoka, Suzumi M.
Hamano, Fumie
Yamazaki, Maya
Sakimura, Kenji
Kano, Masanobu
Shimizu, Takao
PLOS ONE, 2015, 10 (07):

← 1 2 3 4 5 →