1186316-75-5Relevant academic research and scientific papers
Fatty acid amide hydrolase inhibitors. 3: Tetra-substituted azetidine ureas with in vivo activity
Roughley, Stephen D.,Browne, Helen,MacIas, Alba T.,Benwell, Karen,Brooks, Teresa,D'Alessandro, Jalanie,Daniels, Zoe,Dugdale, Sarah,Francis, Geraint,Gibbons, Ben,Hart, Terance,Haymes, Timothy,Kennett, Guy,Lightowler, Sean,Matassova, Natalia,Mansell, Howard,Merrett, Angela,Misra, Anil,Padfield, Anthony,Parsons, Rachel,Pratt, Robert,Robertson, Alan,Simmonite, Heather,Tan, Kiri,Walls, Steven B.,Wong, Melanie
, p. 901 - 906 (2012/03/11)
We describe here our attempts to optimise the human fatty acid amide hydrolase (FAAH) inhibition and physicochemical properties of our previously reported tetrasubstituted azetidine urea FAAH inhibitor, VER-156084. We describe the SAR of a series of analogues and conclude with the demonstration of in vivo dose-dependant FAAH inhibition in an anandamide-loading study in rats.
Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas
Hart, Terance,Macias, Alba T.,Benwell, Karen,Brooks, Teresa,D'Alessandro, Jalanie,Dokurno, Pawel,Francis, Geraint,Gibbons, Ben,Haymes, Timothy,Kennett, Guy,Lightowler, Sean,Mansell, Howard,Matassova, Natalia,Misra, Anil,Padfield, Anthony,Parsons, Rachel,Pratt, Robert,Robertson, Alan,Walls, Steven,Wong, Melanie,Roughley, Stephen
supporting information; experimental part, p. 4241 - 4244 (2010/04/02)
We report the discovery of a novel, chiral azetidine urea inhibitor of Fatty Acid Amide Hydrolase (FAAH,) and describe the surprising species selectivity of VER-156084 versus rat and human FAAH and also hCB1.
