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A reversible and se...
A reversible and selective inhibitor of monoacylglycerol lipase ameliorates multiple sclerosis
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Hernández-Torres, Gloria (author)
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- Cipriano, Mariateresa (author)
- Umeå universitet,Farmakologi
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- Hedén, Erika (author)
- Umeå universitet,Klinisk neurovetenskap
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- Björklund, Emmelie (author)
- Umeå universitet,Farmakologi
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Canales, Ángeles (author)
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Zian, Debora (author)
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Feliú, Ana (author)
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Mecha, Miriam (author)
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Guaza, Carmen (author)
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- Fowler, Christopher J. (author)
- Umeå universitet,Farmakologi
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Ortega-Gutiérrez, Silvia (author)
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López-Rodríguez, María L. (author)
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(creator_code:org_t)
- 2014-10-08
- 2014
- English.
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In: Angewandte Chemie International Edition. - : Wiley-VCH Verlagsgesellschaft. - 1433-7851 .- 1521-3773. ; 53:50, s. 13765-13770
- Related links:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Subject headings
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- Monoacylglycerol lipase (MAGL) is the enzyme responsible for the inactivation of the endocannabinoid 2-arachidonoylglycerol (2-AG). MAGL inhibitors show analgesic and tissue-protecting effects in several disease models. However, the few efficient and selective MAGL inhibitors described to date block the enzyme irreversibly, and this can lead to pharmacological tolerance. Hence, additional classes of MAGL inhibitors are needed to validate this enzyme as a therapeutic target. Here we report a potent, selective, and reversible MAGL inhibitor (IC50=0.18M) which is active in vivo and ameliorates the clinical progression of a multiple sclerosis (MS) mouse model without inducing undesirable CB1-mediated side effects. These results support the interest in MAGL as a target for the treatment of MS.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinsk bioteknologi -- Medicinsk bioteknologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Medical Biotechnology -- Medical Biotechnology (hsv//eng)
Keyword
- endocannabinoids
- endogenous cannabinoid system
- enzyme inhibitors
- monoacylglycerol lipase
- ltiple sclerosis
Publication and Content Type
- ref (subject category)
- art (subject category)
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Hernández-Torres ...
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Cipriano, Mariat ...
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Hedén, Erika
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Björklund, Emmel ...
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Canales, Ángeles
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Zian, Debora
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show more...
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Feliú, Ana
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Mecha, Miriam
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Guaza, Carmen
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Fowler, Christop ...
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Ortega-Gutiérrez ...
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López-Rodríguez, ...
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Medical Biotechn ...
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and Medical Biotechn ...
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Angewandte Chemi ...
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Umeå University