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Pharmacological characterization of endocannabinoid transport and fatty acid amide hydrolase inhibitors.

التفاصيل البيبلوغرافية
العنوان: Pharmacological characterization of endocannabinoid transport and fatty acid amide hydrolase inhibitors.
المؤلفون: Dickason-Chesterfield AK; Eli Lilly & Company, Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, Indiana 46285, USA., Kidd SR, Moore SA, Schaus JM, Liu B, Nomikos GG, Felder CC
المصدر: Cellular and molecular neurobiology [Cell Mol Neurobiol] 2006 Jul-Aug; Vol. 26 (4-6), pp. 407-23. Date of Electronic Publication: 2006 May 31.
نوع المنشور: Comparative Study; Evaluation Study; Journal Article
اللغة: English
بيانات الدورية: Publisher: Kluwer Academic/Plenum Publishers Country of Publication: United States NLM ID: 8200709 Publication Model: Print-Electronic Cited Medium: Print ISSN: 0272-4340 (Print) Linking ISSN: 02724340 NLM ISO Abbreviation: Cell Mol Neurobiol Subsets: MEDLINE
أسماء مطبوعة: Publication: 1999- : New York : Kluwer Academic/Plenum Publishers
Original Publication: New York : Plenum Press, c1981-
مواضيع طبية MeSH: Endocannabinoids*, Amidohydrolases/*antagonists & inhibitors , Cannabinoid Receptor Modulators/*metabolism, Amidohydrolases/analysis ; Amidohydrolases/metabolism ; Animals ; Arachidonic Acids/analysis ; Arachidonic Acids/metabolism ; Binding, Competitive ; Biological Transport/drug effects ; Cells, Cultured ; HeLa Cells ; Humans ; Models, Biological ; Polyunsaturated Alkamides/analysis ; Polyunsaturated Alkamides/metabolism ; Radioligand Assay ; Rats ; Structure-Activity Relationship ; Substrate Specificity
مستخلص: : 1. The mechanism of anandamide uptake and disposal has been an issue of considerable debate in the cannabinoid field. Several compounds have been reported to inhibit anandamide uptake or fatty acid amide hydrolase (FAAH; the primary catabolic enzyme of anandamide) activity with varying degrees of potency and selectivity. We recently reported the first evidence of a binding site involved in the uptake of endocannabinoids that is independent from FAAH. There are no direct comparisons of purported selective inhibitory compounds in common assay conditions measuring anandamide uptake, FAAH activity and binding activity. 2. A subset of compounds reported in the literature were tested in our laboratory under common assay conditions to measure their ability to (a) inhibit [(14)C]-anandamide uptake in cells containing (RBL-2H3) or cells lacking (HeLa) FAAH, (b) inhibit purified FAAH hydrolytic activity, and (c) inhibit binding to a putative binding site involved in endocannabinoid transport in both RBL and HeLa cell membranes. 3. Under these conditions, nearly all compounds tested inhibited (a) uptake of [(14)C]-anandamide, (b) enzyme activity in purified FAAH preparations, and (c) radioligand binding of [(3)H]-LY2183240 in RBL and HeLa plasma membrane preparations. General rank order potency was preserved within the three assays. However, concentration response curves were right-shifted for functional [(14)C]-anandamide uptake in HeLa (FAAH(-/-)) cells. 4. A more direct comparison of multiple inhibitors could be made in these three assay systems performed in the same laboratory, revealing more information about the selectivity of these compounds and the relationship between the putative endocannabinoid transport protein and FAAH. At least two separate proteins appear to be involved in uptake and degradation of anandamide. The most potent inhibitory compounds were right-shifted when transport was measured in HeLa (FAAH(-/-)) cells suggesting a requirement for a direct interaction with the FAAH protein to maintain high affinity binding of anandamide or inhibitors to the putative anandamide transport protein.
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المشرفين على المادة: 0 (Arachidonic Acids)
0 (Cannabinoid Receptor Modulators)
0 (Endocannabinoids)
0 (Polyunsaturated Alkamides)
EC 3.5.- (Amidohydrolases)
EC 3.5.1.- (fatty-acid amide hydrolase)
UR5G69TJKH (anandamide)
تواريخ الأحداث: Date Created: 20060601 Date Completed: 20070424 Latest Revision: 20191210
رمز التحديث: 20221213
DOI: 10.1007/s10571-006-9072-6
PMID: 16736384
قاعدة البيانات: MEDLINE
الوصف
تدمد:0272-4340
DOI:10.1007/s10571-006-9072-6