PF3845yne

中文名称：

4-[[3-[(5-乙炔基-2-吡啶基)氧基]苯基]甲基]-N-3-吡啶基-1-哌啶甲酰胺

PF-3845 is a fatty acid amide hydrolase (FAAH) inhibitor, and acts in the nervous system to reverse LPS-induced tactile allodynia in mice. PF-3845 promotes neuronal survival, attenuates inflammation and improves functional recovery in mice with traumatic brain injury. Treatment with PF3845 inactivated FAAH activity and enhanced the AEA levels in the brain. It reduced neurodegeneration in the dentate gyrus, and up-regulated the expression of Bcl-2 and Hsp70/72 in both cortex and hippocampus. PF3845 also suppressed the increased production of amyloid precursor protein, prevented dendritic loss and restored the levels of synaptophysin in the ipsilateral dentate gyrus.

1: Ramesh D, Ross GR, Schlosburg JE, Owens RA, Abdullah RA, Kinsey SG, Long JZ, Nomura DK, Sim-Selley LJ, Cravatt BF, Akbarali HI, Lichtman AH. Blockade of endocannabinoid hydrolytic enzymes attenuates precipitated opioid withdrawal symptoms in mice. J Pharmacol Exp Ther. 2011 Oct;339(1):173-85. Epub 2011 Jun 30. PubMed PMID: 21719468; PubMed Central PMCID: PMC3186294.

2: Kinsey SG, Nomura DK, O'Neal ST, Long JZ, Mahadevan A, Cravatt BF, Grider JR, Lichtman AH. Inhibition of monoacylglycerol lipase attenuates nonsteroidal anti-inflammatory drug-induced gastric hemorrhages in mice. J Pharmacol Exp Ther. 2011 Sep;338(3):795-802. Epub 2011 Jun 9. PubMed PMID: 21659471; PubMed Central PMCID: PMC3164340.

3: Booker L, Kinsey SG, Abdullah RA, Blankman JL, Long JZ, Ezzili C, Boger DL, Cravatt BF, Lichtman AH. The FAAH Inhibitor PF-3845 Acts in the Nervous System to Reverse Lipopolysaccharide-induced Tactile Allodynia in Mice. Br J Pharmacol. 2011 Apr 20. doi: 10.1111/j.1476-5381.2011.01445.x. [Epub ahead of print] PubMed PMID: 21506952.