Drug intelligence / Profile preview

Compound 4f

Development stage
Preclinical
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral
01

Overview

Compound 4f is a novel, potent, and reversible monoacylglycerol lipase (MAGL) inhibitor developed by Takeda Pharmaceutical Company. It is designed as a brain-penetrant small molecule that targets the degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG) into arachidonic acid, thereby modulating neuroinflammatory pathways. By inhibiting MAGL, Compound 4f increases 2-AG levels and reduces the production of pro-inflammatory prostaglandins. In preclinical models, it has demonstrated significant neuroprotective and anti-inflammatory effects, showing efficacy in reducing neuronal cell loss and cognitive impairment. The compound is characterized by high selectivity over other serine hydrolases such as fatty acid amide hydrolase (FAAH) and alpha/beta-hydrolase domain-containing protein 6 (ABHD6).

Other names
(2S,4S)-2-((3-((3-chloro-4-methylbenzyl)oxy)azetidine-1-yl)carbonyl)-7-oxa-5-azaspiro[3.4]octan-6-one
02

Targets

HTR2B (5-Hydroxytryptamine Receptor 2B)σR (Sigma receptors)MAOB (Monoamine oxidase B)MGLL (Monoacylglycerol lipase)

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