2006
DOI: 10.1016/j.bbalip.2005.12.009
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Development of the first potent and specific inhibitors of endocannabinoid biosynthesis

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Cited by 118 publications
(110 citation statements)
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References 27 publications
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“…4 b and c and previous evidence (18) suggest that the three eCB pathways are not identical. Because THL antagonizes lipase activities downstream of Ca 2ϩ (24), these experiments are compatible with the concept that a rise in [Ca 2ϩ ] i primes cells independently of DGL. Moreover, the priming mechanism appears to be distinct from the Ca 2ϩ -dependent and eCB mAChR pathways.…”
Section: Priming Of Mglur-mediated Ecb Mobilizationsupporting
confidence: 72%
See 1 more Smart Citation
“…4 b and c and previous evidence (18) suggest that the three eCB pathways are not identical. Because THL antagonizes lipase activities downstream of Ca 2ϩ (24), these experiments are compatible with the concept that a rise in [Ca 2ϩ ] i primes cells independently of DGL. Moreover, the priming mechanism appears to be distinct from the Ca 2ϩ -dependent and eCB mAChR pathways.…”
Section: Priming Of Mglur-mediated Ecb Mobilizationsupporting
confidence: 72%
“…S2). RHC 80267 is a comparatively weak DGL inhibitor in biochemical assays whereas tetrahydrolipstatin, tetrahydrolipstatin (THL; orlistat), is more potent (24), and it inhibits some eCB responses (18,(25)(26)(27). We found that extracellular application of 10 M THL reduced DSI and virtually abolished the carbachol (CCh)-induced eCB mAChR response without preventing eCB mGluR priming (Fig.…”
Section: Priming Of Mglur-mediated Ecb Mobilizationmentioning
confidence: 86%
“…Cultured neurons were maintained in DMEM/F12, supplemented with 1% B27/1% glutamine/1% penicillin/streptomycin for 3-6 days (7). Ligands were first added 12 h after cell seeding and replenished every other day (7), except for O-3841 (1 M) (19), which was used between days 2-6 in vitro. Density of glutamatergic neurons was defined as a ratio of VGLUT1 ϩ /TuJ1 ϩ cells from Ն10 randomly selected view fields per coverslip.…”
Section: Methodsmentioning
confidence: 99%
“…6,7 In recent years a few novel MGL inhibitors were discovered. 4,[8][9][10][11] Until recently, the only selective small-molecule inhibitor of MGL was URB602 (FIG. 1), a carbamate derivative possessing a moderate activity (half-maximal inhibitory concentration, IC 50 = 75±7 µM in rat brain MGL expressed in HeLa cells and 28±4 µM in native rat brain MGL).…”
Section: Introductionmentioning
confidence: 99%