PF-3845 Inhibitor CAS No. 1196109-52-0

Cat. No.	Name	Size	Price
KI0557	PF-3845	10 mg	$192
	PF-3845	50 mg	$752
	PF-3845	200 mg	$2032

Chemical Characteristic

Product Name	PF-3845
CAS No.	1196109-52-0
Molecular Weight	456
Formula	C₂₄H₂₃F₃N₄O₂
Chemical Name	N-3-Pyridinyl-4-[[3-[[5-(trifluoromethyl)-2-pyridinyl]oxy]phenyl]methyl]-1-piperidinecarboxamide
Smiles	N1(CCC(CC1)Cc1cc(ccc1)Oc1ccc(cn1)C(F)(F)F)C(=O)Nc1cnccc1
Chemical Structure

Biological activities

PF-3845 is a fatty acid amide hydrolase (FAAH) inhibitor. The Ki of PF-3845 is 0.23 μM against FAAH. PF-3845-treated mice (10 mg/kg, i.p.) also reveal dramatic (> 10-fold) elevations in brain levels of AEA and other NAEs [N-pamitoyl ethanolamine (PEA) and N-oleoyl ethanolamine (OEA). PF-3845 [1 ??30 mg/kg, oral administration (p.o),] dose-dependently inhibits mechanical allodynia with a minimum effective dose (MED) of 3 mg/kg (rats are analyzed at 4 hours post-dosing with PF-3845).^[1] i.p. PF-3845 increases AEA levels in the brain and spinal cord. Additionally, intraplantar PF-3845 produces a partial reduction in allodynia.^[2] PF-3845 significantly reverses LPS-induced tactile allodynia. Intraplantar administration of PF-3845 (1, 3 or 10 µg) partially reverses allodynia in the LPS administered paw. Systemic administration of PF-3845 (10 mg/kg) or i.pl. injection of a much higher dose of PF-3845 (i.e. 10 µg) causes significant increases in AEA, but not 2-AG levels in the brain and spinal cord.^[2] PF-3845 lacks anti-allodynic efficacy in knockout CB_{1 (-/-) mice.^[3]}

References

[1] Ahn K, et al. Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain. Chem Biol. 2009, 16(4): 411-420. [2] Booker L, et al. The fatty acid amide hydrolase (FAAH) inhibitor PF-3845 acts in the nervous system to reverse LPS-induced tactile allodynia in mice. Br J Pharmacol. 2012, 165(8): 2485-2496. [3] Kinsey SG, et al. Fatty acid amide hydrolase and monoacylglycerol lipase inhibitors produce anti-allodynic effects in mice through distinct cannabinoid receptor mechanisms. J Pain. 2010, 11(12): 1420-1428.

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