Preferred Label : Elcubragistat;
NCIt synonyms : MGLL Inhibitor ABX-1431; Serine Hydrolase Monoacylglycerol Lipase Inhibitor ABX-1431;
NCIt definition : An orally bioavailable inhibitor of the serine hydrolase monoacylglycerol lipase (MGLL),
with potential use for the treatment of various central nervous system (CNS) diseases
and with potential analgesic and anti-neuroinflammatory activities. Upon oral administration,
elcubragistat targets and binds to MGLL, thereby inhibiting MGLL activity and preventing
the breakdown and inactivation of endogenous 2-arachidonoylglycerol (2-AG). Increased
2-AG levels results in enhanced activation of the cannabinoid receptor 1 (CB1) in
the CNS and enhanced CB1 endocannabinoid signaling in active neural circuits. Activation
of CB1 helps modulate the endocannabinoid system and reduce neurotransmitter release,
thereby decreasing overactive neural signaling. This induces analgesic, anti-inflammatory
and various neurological effects that are caused by dysregulation of the endocannabinoid
system and overactive neural signaling, including anxiolytic effects, reduced spasticity
and decreased neurodegenerative effects. In addition, MGLL inhibition by elcubragistat
depletes the supply of the inflammatory signaling molecule arachidonic acid, thereby
further alleviating pain and inflammation. CB1 plays a key role in the regulation
of neurotransmission; increased CB1 activation decreases overactive neural signaling.
MGLL, an enzyme that catalyzes the breakdown of 2-AG, regulates the activation of
CB1 and CB2 to modulate neurotransmission and inflammatory signaling, respectively.;
UNII : FB39E94UXK;
CAS number : 1446817-84-0;
Molecule name : ABX-1431;
NCI Metathesaurus CUI : CL551127;
Origin ID : C148538;
UMLS CUI : C5706634;
Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
