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Molecular characterization of an enzyme that degrades neuromodulatory fatty-acid amides
TLDR
It is shown that oleamide hydrolase may serve as the general inactivating enzyme for a growing family of bioactive signalling molecules, the fatty-acid amides6–8, and the structure and sleep-inducing properties of cis-9-octadecenamide, a lipid isolated from the cerebrospinal fluid of sleep-deprived cats are reported. Expand
Reliability of Spike Timing in Neocortical Neurons
screen of the microscope. Between 150 to 300 nerve fibers were analyzed per cross section. 13. C. F. Eldridge, M. Bartlett, R. P. Bunge, P. M. Wood, J. Cell Biol. 105, 1023 (1987); C. F. Eldridge, M.Expand
Reversible Inhibitors of Fatty Acid Amide Hydrolase That Promote Analgesia: Evidence for an Unprecedented Combination of Potency and Selectivity
TLDR
A class of α-keto-heterocycles are identified that show unprecedented selectivity for FAAH relative to other mammalian hydrolases, and, when administered to rodents, raise central nervous system levels of anandamide and promote cannabinoid receptor 1-dependent analgesia in several assays of pain sensation. Expand
Blockade of Endocannabinoid-Degrading Enzymes Attenuates Neuropathic Pain
TLDR
The data indicate that inhibition of FAAH and MAGL reduces neuropathic pain through distinct receptor mechanisms of action and present viable targets for the development of analgesic therapeutics. Expand
The Sleep-inducing Lipid Oleamide Deconvolutes Gap Junction Communication and Calcium Wave Transmission in Glial Cells
TLDR
Oleamide- induced inactivation of glial cell gap junction channels may serve to regulate communication between brain cells, and in doing so, may influence higher order neuronal events like sleep induction. Expand
Chemical characterization of a family of brain lipids that induce sleep.
TLDR
Results suggest that fatty acid primary amides may represent a previously unrecognized class of biological signaling molecules. Expand
A simple, high-resolution method for establishing DNA binding affinity and sequence selectivity.
TLDR
Techniques for establishing binding constants from quantitative titrations are compared, and recommendations are made for use of a Scatchard or curve fitting analysis of the titration binding curves as a reliable means to quantitate the binding affinity. Expand
Exceptionally potent inhibitors of fatty acid amide hydrolase: the enzyme responsible for degradation of endogenous oleamide and anandamide.
TLDR
The development of exceptionally potent inhibitors of fatty acid amide hydrolase (FAAH), the enzyme responsible for the degradation of oleamide, and anandamide (an endogenous ligand for cannabinoid receptors) is detailed. Expand
Discovery of a potent, selective, and efficacious class of reversible alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase effective as analgesics.
TLDR
The discovery of a potent, selective, and efficacious class of reversible FAAH inhibitors that produce analgesia in animal models validating a new therapeutic target for pain intervention is reported. Expand
Small-molecule antagonists of Myc/Max dimerization inhibit Myc-induced transformation of chicken embryo fibroblasts
TLDR
This work provides proof of principle for the identification of small molecule inhibitors of protein–protein interactions by using high-throughput screens of combinatorial chemical libraries. Expand
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