| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| Cristiano Ruch Werneck Guimarães, Dale L Boger, William L Jorgense. Elucidation of fatty acid amide hydrolase inhibition by potent alpha-ketoheterocycle derivatives from Monte Carlo simulations. Journal of the American Chemical Society. vol 127. issue 49. 2006-02-22. PMID:16332087. |
fatty acid amide hydrolase (faah) is a serine hydrolase responsible for the degradation of anandamide, an endogenous cannabinoid agonist, and oleamide, a sleep-inducing lipid. |
2006-02-22 |
2023-08-12 |
Not clear |
| Giulio G Muccioli, Nicola Fazio, Gerhard K E Scriba, Wolfgang Poppitz, Fabio Cannata, Jacques H Poupaert, Johan Wouters, Didier M Lamber. Substituted 2-thioxoimidazolidin-4-ones and imidazolidine-2,4-diones as fatty acid amide hydrolase inhibitors templates. Journal of medicinal chemistry. vol 49. issue 1. 2006-02-16. PMID:16392827. |
in the present study, we synthesized several derivatives exhibiting interesting faah inhibitory activity and devoid of affinity for the cb(1) and cb(2) cannabinoid receptors. |
2006-02-16 |
2023-08-12 |
Not clear |
| Giulio G Muccioli, Nicola Fazio, Gerhard K E Scriba, Wolfgang Poppitz, Fabio Cannata, Jacques H Poupaert, Johan Wouters, Didier M Lamber. Substituted 2-thioxoimidazolidin-4-ones and imidazolidine-2,4-diones as fatty acid amide hydrolase inhibitors templates. Journal of medicinal chemistry. vol 49. issue 1. 2006-02-16. PMID:16392827. |
in conclusion, it appears that even though several 3-substituted 5,5'-diphenyl-2-thioxoimidazolidin-4-one and 3-substituted 5,5'-diphenylimidazolidine-2,4-dione derivatives have been previously shown to behave as cb(1) cannabinoid receptor ligands, appropriate substitutions of these templates can result in faah inhibitors devoid of affinity for the cannabinoid receptors. |
2006-02-16 |
2023-08-12 |
Not clear |
| Alessia Ligresti, Maria Grazia Cascio, Vincenzo Di Marz. Endocannabinoid metabolic pathways and enzymes. Current drug targets. CNS and neurological disorders. vol 4. issue 6. 2006-02-07. PMID:16375679. |
five endocannabinoid enzymes have been cloned to date: two are responsible for the biosynthesis and degradation of anandamide, the nape-selective phospholipase d and the fatty acid amide hydrolase, respectively; the other three catalyse the biosynthesis and degradation of 2-ag, the sn-1-selective diacylglycerol lipases alpha and beta and the monoacylglycerol lipase, respectively. |
2006-02-07 |
2023-08-12 |
human |
| Enrico Dainese, Valeria Gasperi, Mauro Maccarron. Partial QSAR analysis of some selected natural inhibitors of FAAH suggests a working hypothesis for the development of endocannabinoid-based drugs. Current drug targets. CNS and neurological disorders. vol 4. issue 6. 2006-02-07. PMID:16375688. |
the discovery of n-arachidonoylethanolamine (anandamide, aea) and of the enzyme that terminates its signaling, i. e. fatty acid amide hydrolase (faah), has inspired pharmacological strategies to augment endocannabinoid tone and biological activity through inhibition of faah. |
2006-02-07 |
2023-08-12 |
Not clear |
| Enrico Dainese, Valeria Gasperi, Mauro Maccarron. Partial QSAR analysis of some selected natural inhibitors of FAAH suggests a working hypothesis for the development of endocannabinoid-based drugs. Current drug targets. CNS and neurological disorders. vol 4. issue 6. 2006-02-07. PMID:16375688. |
here we discuss the role of natural endocannabinoid derivatives, like the hydroxy-anandamides (oh-aeas) generated from aea via lipoxygenase activity, as powerful inhibitors of faah. |
2006-02-07 |
2023-08-12 |
Not clear |
| Enrico Dainese, Valeria Gasperi, Mauro Maccarron. Partial QSAR analysis of some selected natural inhibitors of FAAH suggests a working hypothesis for the development of endocannabinoid-based drugs. Current drug targets. CNS and neurological disorders. vol 4. issue 6. 2006-02-07. PMID:16375688. |
we propose that these compounds, by reversibly inhibiting faah, may control in vivo the endocannabinoid tone. |
2006-02-07 |
2023-08-12 |
Not clear |
| Mauro Maccarrone, Barbara Barboni, Andrea Paradisi, Nicola Bernabò, Valeria Gasperi, Maria Gabriella Pistilli, Filomena Fezza, Pia Lucidi, Mauro Mattiol. Characterization of the endocannabinoid system in boar spermatozoa and implications for sperm capacitation and acrosome reaction. Journal of cell science. vol 118. issue Pt 19. 2006-01-27. PMID:16144868. |
type-1 cannabinoid receptors (cb1r), vanilloid receptors (trpv1), aea-synthesizing phospholipase d (nape-pld), aea transporter (amt) and aea hydrolase (faah). |
2006-01-27 |
2023-08-12 |
Not clear |
| Séverine Vandevoorde, Christopher J Fowle. Inhibition of fatty acid amide hydrolase and monoacylglycerol lipase by the anandamide uptake inhibitor VDM11: evidence that VDM11 acts as an FAAH substrate. British journal of pharmacology. vol 145. issue 7. 2006-01-17. PMID:15895107. |
there is some dispute concerning the extent to which the uptake inhibitor vdm11 (n-(4-hydroxy-2-methylphenyl) arachidonoyl amide) is capable of inhibiting the metabolism of the endocannabinoid anandamide (aea) by fatty acid amide hydrolase (faah). |
2006-01-17 |
2023-08-12 |
rat |
| Antonella Brizzi, Vittorio Brizzi, Maria Grazia Cascio, Tiziana Bisogno, Rossella Sirianni, Vincenzo Di Marz. Design, synthesis, and binding studies of new potent ligands of cannabinoid receptors. Journal of medicinal chemistry. vol 48. issue 23. 2006-01-17. PMID:16279794. |
binding studies on cb1 and cb2 receptors, anandamide membrane transporter (amt), and fatty acid amide hydrolase (faah) showed that some of the newly developed compounds have high affinity and specificity for cannabinoid cb1 and cb2 receptors. |
2006-01-17 |
2023-08-12 |
Not clear |
| Alan Saghatelian, Benjamin F Cravat. Discovery metabolite profiling--forging functional connections between the proteome and metabolome. Life sciences. vol 77. issue 14. 2006-01-05. PMID:15964030. |
we have applied dmp to study mice lacking the enzyme fatty acid amide hydrolase (faah), which degrades the endocannabinoid family of signaling lipids. |
2006-01-05 |
2023-08-12 |
mouse |
| Yong-Xin Sun, Kazuhito Tsuboi, Li-Ying Zhao, Yasuo Okamoto, Didier M Lambert, Natsuo Ued. Involvement of N-acylethanolamine-hydrolyzing acid amidase in the degradation of anandamide and other N-acylethanolamines in macrophages. Biochimica et biophysica acta. vol 1736. issue 3. 2005-12-16. PMID:16154384. |
bioactive n-acylethanolamines including the endocannabinoid anandamide are known to be hydrolyzed to fatty acids and ethanolamine by fatty acid amide hydrolase (faah). |
2005-12-16 |
2023-08-12 |
mouse |
| Nissar A Darmani, Bryan A McClanahan, Chung Trinh, Stefania Petrosino, Marta Valenti, Vincenzo Di Marz. Cisplatin increases brain 2-arachidonoylglycerol (2-AG) and concomitantly reduces intestinal 2-AG and anandamide levels in the least shrew. Neuropharmacology. vol 49. issue 4. 2005-12-07. PMID:15921709. |
of one of the major endocannabinoid metabolic enzymes, the intracellular fatty acid amide hydrolase (faah), do not significantly prevent vomiting produced by emetic doses of i.p.-administered 2-ag, cisplatin or the dopamine receptor agonist apomorphine. |
2005-12-07 |
2023-08-12 |
Not clear |
| Stefan Engeli, Jana Böhnke, Mareike Feldpausch, Kerstin Gorzelniak, Jürgen Janke, Sándor Bátkai, Pál Pacher, Judy Harvey-White, Friedrich C Luft, Arya M Sharma, Jens Jorda. Activation of the peripheral endocannabinoid system in human obesity. Diabetes. vol 54. issue 10. 2005-11-30. PMID:16186383. |
we measured circulating endocannabinoid concentrations and studied the expression of cb-1 and the main degrading enzyme, fatty acid amide hydrolase (faah), in adipose tissue of lean (n = 20) and obese (n = 20) women and after a 5% weight loss in a second group of women (n = 17). |
2005-11-30 |
2023-08-12 |
human |
| Douglas Osei-Hyiaman, Michael Depetrillo, Judith Harvey-White, Anthony W Bannon, Benjamin F Cravatt, Michael J Kuhar, Ken Mackie, Miklós Palkovits, George Kuno. Cocaine- and amphetamine-related transcript is involved in the orexigenic effect of endogenous anandamide. Neuroendocrinology. vol 81. issue 4. 2005-10-31. PMID:16131814. |
mice deficient in fatty acid amide hydrolase (faah), the enzyme responsible for the in vivo metabolism of the endocannabinoid anandamide, have reduced levels of cart-immunoreactive nerve fibers and terminals in several brain regions implicated in appetite control, including the arcuate, dorsomedial and periventricular nuclei of the hypothalamus, the amygdala, the bed nucleus of the stria terminalis and the nucleus accumbens, and treatment of faah(-/-) mice with rimonabant, 3 mg/kg/day for 7 days, increased cart levels toward those seen in faah(+/+) wild-type controls. |
2005-10-31 |
2023-08-12 |
mouse |
| Michele K McKinney, Benjamin F Cravat. Structure and function of fatty acid amide hydrolase. Annual review of biochemistry. vol 74. 2005-09-29. PMID:15952893. |
fatty acid amide hydrolase (faah) is a mammalian integral membrane enzyme that degrades the fatty acid amide family of endogenous signaling lipids, which includes the endogenous cannabinoid anandamide and the sleep-inducing substance oleamide. |
2005-09-29 |
2023-08-12 |
human |
| Marc Steffens, Andreas Schulze-Bonhage, Rainer Surges, Thomas J Feuerstei. Fatty acid amidohydrolase in human neocortex-activity in epileptic and non-epileptic brain tissue and inhibition by putative endocannabinoids. Neuroscience letters. vol 385. issue 1. 2005-09-23. PMID:15923084. |
to further increase endocannabinoid activity, the application of faah inhibitors might be therapeutically useful in the treatment of neuronal hyperexcitability. |
2005-09-23 |
2023-08-12 |
human |
| Diane L Lynch, Patricia H Reggi. Molecular dynamics simulations of the endocannabinoid N-arachidonoylethanolamine (anandamide) in a phospholipid bilayer: probing structure and dynamics. Journal of medicinal chemistry. vol 48. issue 15. 2005-08-23. PMID:16033262. |
compound 1 has been shown to be synthesized from lipids, to interact with the membrane-embedded cannabinoid cb1 receptor, to be transported to intracellular compartments, possibly via caveolae-related endocytosis, and finally, to be degraded by fatty acid amide hydrolase (faah), an integral membrane protein which has an active site that is accessed by 1 possibly via the bilayer. |
2005-08-23 |
2023-08-12 |
Not clear |
| Diane L Lynch, Patricia H Reggi. Molecular dynamics simulations of the endocannabinoid N-arachidonoylethanolamine (anandamide) in a phospholipid bilayer: probing structure and dynamics. Journal of medicinal chemistry. vol 48. issue 15. 2005-08-23. PMID:16033262. |
the bilayer location for 1 revealed by these studies may be important for the interaction of 1 with membrane-embedded proteins such as the cannabinoid cb1 receptor and membrane-associated proteins such as faah. |
2005-08-23 |
2023-08-12 |
Not clear |
| Eva de Lago, Stefania Petrosino, Marta Valenti, Enrico Morera, Silvia Ortega-Gutierrez, Javier Fernandez-Ruiz, Vincenzo Di Marz. Effect of repeated systemic administration of selective inhibitors of endocannabinoid inactivation on rat brain endocannabinoid levels. Biochemical pharmacology. vol 70. issue 3. 2005-08-18. PMID:15963472. |
several selective inhibitors of endocannabinoid inactivation via either the fatty acid amide hydrolase (faah) or the putative endocannabinoid transporter have been developed so far. |
2005-08-18 |
2023-08-12 |
rat |