U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



PF-3845 is a selective covalent inhibitor of fatty acid amide hydrolase. It results in increased levels of anandamide and results in cannabinoid receptor-based effects. PF-3845 demonstrated cannabinoid receptor-dependent antinociceptive effects in models of inflammatory and neuropathic pain. In mouse model PF-3845 attenuated withdrawal from morphine dependence. PF3845 reversed traumatic brain injury (TBI)-induced impairments in fine motor movement, hippocampus dependent working memory and anxiety-like behavior in a tramatic brain injury model.
CX614 (2H,3H,6aH-pyrrolidino(2,1-3',2')1,3-oxazino(6',5'-5,4)benzo(e)1,4-dioxan-10-one) is a positive allosteric modulator of the AMPA receptor. Chronic treatment of rat hippocampal slices with CX614 gradually reduced levels of glutamate receptor (GluR)1 and GluR2/3 AMPA subunits and of their anchoring proteins synapse-associated protein 97 (SAP97) and glutamate receptor interacting protein 1 (GRIP1). The physiological and toxicological properties of this compound have not been evaluated in humans.