Antinociceptive activity of the endogenous fatty acid amide, palmitylethanolamide
نویسندگان
چکیده
منابع مشابه
Luciferin Amides Enable in Vivo Bioluminescence Detection of Endogenous Fatty Acid Amide Hydrolase Activity
Firefly luciferase is homologous to fatty acyl-CoA synthetases. We hypothesized that the firefly luciferase substrate d-luciferin and its analogs are fatty acid mimics that are ideally suited to probe the chemistry of enzymes that release fatty acid products. Here, we synthesized luciferin amides and found that these molecules are hydrolyzed to substrates for firefly luciferase by the enzyme fa...
متن کاملFatty Acid Amide Hydrolase-Dependent Generation of Antinociceptive Drug Metabolites Acting on TRPV1 in the Brain
The discovery that paracetamol is metabolized to the potent TRPV1 activator N-(4-hydroxyphenyl)-5Z,8Z,11Z,14Z-eicosatetraenamide (AM404) and that this metabolite contributes to paracetamol's antinociceptive effect in rodents via activation of TRPV1 in the central nervous system (CNS) has provided a potential strategy for developing novel analgesics. Here we validated this strategy by examining ...
متن کاملRole of fatty acid amide hydrolase in the transport of the endogenous cannabinoid anandamide.
A facilitated transport process that removes the endogenous cannabinoid anandamide from extracellular spaces has been identified. Once transported into the cytoplasm, fatty acid amide hydrolase (FAAH) is responsible for metabolizing the accumulated anandamide. We propose that FAAH contributes to anandamide uptake by creating and maintaining an inward concentration gradient for anandamide. To ex...
متن کاملACCELERATED COMMUNICATION Role of Fatty Acid Amide Hydrolase in the Transport of the Endogenous Cannabinoid Anandamide
A facilitated transport process that removes the endogenous cannabinoid anandamide from extracellular spaces has been identified. Once transported into the cytoplasm, fatty acid amide hydrolase (FAAH) is responsible for metabolizing the accumulated anandamide. We propose that FAAH contributes to anandamide uptake by creating and maintaining an inward concentration gradient for anandamide. To ex...
متن کاملMapping human brain fatty acid amide hydrolase activity with PET.
Endocannabinoid tone has recently been implicated in a number of prevalent neuropsychiatric conditions. [(11)C]CURB is the first available positron emission tomography (PET) radiotracer for imaging fatty acid amide hydrolase (FAAH), the enzyme which metabolizes the prominent endocannabinoid anandamide. Here, we sought to determine the most suitable kinetic modeling approach for quantifying [(11...
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ژورنال
عنوان ژورنال: European Journal of Pharmacology
سال: 2001
ISSN: 0014-2999
DOI: 10.1016/s0014-2999(01)00988-8