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Selective blockade of the hydrolysis of the endocannabinoid 2-arachidonoylglycerol impairs learning and memory performance while producing antinociceptive activity in rodents.

Griebel G, Pichat P, Beeské S, Leroy T, Redon N, Jacquet A, Françon D, Bert L, Even L, Lopez-Grancha M, Tolstykh T, Sun F, Yu Q, Brittain S, Arlt H, He T, Zhang B, Wiederschain D, Bertrand T, Houtmann J, Rak A, Vallée F, Michot N, Augé F, Menet V, Bergis OE, George P, Avenet P, Mikol V, Didier M, Escoubet J
Sci Rep 5 7642 (2015)
Cited: 53 times
EuropePMC logo PMID: 25560837

Abstract

Monoacylglycerol lipase (MAGL) represents a primary degradation enzyme of the endogenous cannabinoid (eCB), 2-arachidonoyglycerol (2-AG). This study reports a potent covalent MAGL inhibitor, SAR127303. The compound behaves as a selective and competitive inhibitor of mouse and human MAGL, which potently elevates hippocampal levels of 2-AG in mice. In vivo, SAR127303 produces antinociceptive effects in assays of inflammatory and visceral pain. In addition, the drug alters learning performance in several assays related to episodic, working and spatial memory. Moreover, long term potentiation (LTP) of CA1 synaptic transmission and acetylcholine release in the hippocampus, two hallmarks of memory function, are both decreased by SAR127303. Although inactive in acute seizure tests, repeated administration of SAR127303 delays the acquisition and decreases kindled seizures in mice, indicating that the drug slows down epileptogenesis, a finding deserving further investigation to evaluate the potential of MAGL inhibitors as antiepileptics. However, the observation that 2-AG hydrolysis blockade alters learning and memory performance, suggests that such drugs may have limited value as therapeutic agents.

Reviews - 4uuq mentioned but not cited (2)

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Articles - 4uuq mentioned but not cited (3)

  1. Selective blockade of the hydrolysis of the endocannabinoid 2-arachidonoylglycerol impairs learning and memory performance while producing antinociceptive activity in rodents. Griebel G, Pichat P, Beeské S, Leroy T, Redon N, Jacquet A, Françon D, Bert L, Even L, Lopez-Grancha M, Tolstykh T, Sun F, Yu Q, Brittain S, Arlt H, He T, Zhang B, Wiederschain D, Bertrand T, Houtmann J, Rak A, Vallée F, Michot N, Augé F, Menet V, Bergis OE, George P, Avenet P, Mikol V, Didier M, Escoubet J. Sci Rep 5 7642 (2015)
  2. Discovery of 8-prenylnaringenin from hop (Humulus lupulus L.) as a potent monoacylglycerol lipase inhibitor for treatments of neuroinflammation and Alzheimer's disease. Tung MC, Fung KM, Hsu HM, Tseng TS. RSC Adv 11 31062-31072 (2021)
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  1. Therapeutic endocannabinoid augmentation for mood and anxiety disorders: comparative profiling of FAAH, MAGL and dual inhibitors. Bedse G, Bluett RJ, Patrick TA, Romness NK, Gaulden AD, Kingsley PJ, Plath N, Marnett LJ, Patel S. Transl Psychiatry 8 92 (2018)
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