Anandamide transporter

ANANDAMIDE TRANSPORT INHIBITORS The Hydrophobic Chain The Carboxamide/Carboxylate Group The Polar Head Group... [Pg.207]

Anandamide is inactivated in two steps, first by transport inside the cell and subsequently by intracellular enzymatic hydrolysis. The transport of anandamide inside the cell is a carrier-mediated activity, having been shown to be a saturable, time- and temperature-dependent process that involves some protein with high affinity and specificity for anandamide (Beltramo, 1997). This transport process, unlike that of classical neurotransmitters, is Na+-independent and driven only by the concentration gradient of anandamide (Piomelli, 1998). Although the anandamide transporter protein has not been cloned yet, its well characterized activity is known to be inhibited by specific transporter inhibitors. Reuptake of 2-AG is probably mediated by the same facilitating mechanism (Di Marzo, 1999a,b Piomelli, 1999). [Pg.109]

Figure 6 Anandamide metabolism NAPE, N-arachidonylphosphatidyl-ethanol-amides PLD, phospholipase D AEA, anandamide AC, anandamide carrier protein AT, anandamide transporter AEAase, anandamide amidase AA, arachidonic acid.

Beltramo M, Stella N, Calignano A, Lin S, Makriyannis A, Piomelli D. Functional role of high-affinity anandamide transport, as revealed by selective inhibition. Science 1997 277 1094-1097. [Pg.127]

Piomelli D, Beltramo M, Glasnapp S, Lin SY, Goutopoulos A, Xie XQ, Makriyannis A. Structural determinants for recognition and translocation by the anandamide transporter. Proc Natl Acad Sci USA 1999 10 5802-5807. [Pg.134]

Glaser ST, Abumrad NA, Fatade F, Kaczocha M, Studholme KM, Deutsch DG (2003) Evidence against the presence of an anandamide transporter. Proc Natl Acad Sci USA 100(7) 4269-74 Glass M, Felder CC (1997) Concurrent stimulation of cannabinoid CB1 and dopamine D2 receptors augments cAMP accumulation in striatal neurons evidence for a Gs linkage to the CB1 receptor. J Neurosci 17(14) 5327-33... [Pg.470]

Fegley, D., Kathuria, S., Mercier, R., Li, C., Goutopoulos, A., Makriyannis, A., and Piomelli, D. (2004). Anandamide transport is independent of fatty-acid amide hydrolase activity and is blocked by the hydrolysis-resistant inhibitor AMI 172. Proc. Natl. Acad. Sci. USA 101, 8756—8761. [Pg.68]

Structural determinants for recognition and translocation by the anandamide transporter. [Pg.70]

Olvanil (= A-(Vanillyl)-9-oleamide] (vanilloid phenolic) Cholecystokinin receptor Synthetic (cf. Capsaicin) Anandamide transport inhibition [14] (VR agonist) 5.8D... [Pg.219]

Basavarajappa BS, Saito M, Cooper TB, Hungund BL (2003) Chronic ethanol inhibits the anandamide transport and increases extracellular anandamide levels in cerebellar granule neurons. Eur J Pharmacol 466 73-83... [Pg.17]

McFarland MJ, Barker EL (2004) Anandamide transport. Pharmacol Ther 104 117-135... [Pg.22]

Ortega-Gutierrez S, Hawkins EG, Viso A, Lopez-Rodriguez ML, Cravatt BF (2004) Comparison of anandamide transport in FAAH wild-type and knockout neurons evidence for contributions by both FAAH and the CBI receptor to anandamide uptake. Biochemistry 43 8184-8190... [Pg.23]

Jarrahian A, Manna S, Edgemond WS, Campbell WB, Hillard CJ (2000) Structure-activity relationships among N-arachidonylethanolamine (anandamide) head group analogues for the anandamide transporter. J Neurochem 74 2597-2606... [Pg.44]

Reggio PH, Traore H (2000) Conformational requirements for endocannabinoid interaction with the cannabinoid receptors, the anandamide transporter and fatty acid amidohydrolase. Chem Phys Lipids 108 15-35... [Pg.76]

De Petrocellis L, Bisogno T, Davis JB, Pertwee RG, Di Marzo V (2000) Overlap between the ligand recognition properties of the anandamide transporter and the VRl vanilloid receptor inhibitors of anandamide uptake with negligible capsaicin-like activity. FEBS Lett 483 52-56... [Pg.176]

Glaser ST, Abumrad NA, Fatade F, Kaczocha M, Studholme KM, Deutsch DG (2003) Evidence against the presence of an anandamide transporter. Proc Natl Acad Sci USA 100 4269-4274... [Pg.178]

Zygmunt PM, Chuang H, Movahed P, Julius D, Hogestatt ED (2000) The anandamide transport inhibitor AM404 activates vanilloid receptors. Eur J Pharmacol 396 39-42... [Pg.185]

Extensive studies on the endocannabinoid system have revealed a number of cannabinergic proteins involved in the inactivation and biosynthesis of endocannabinoids. These include fatty acid amide hydrolase (FAAH) (Di Marzo et al. 1994 Gaetani et al. 2003 Piomelli et al. 1999), monoglyceride lipase (MAG) (Dinh et al. 2002), and the anandamide transporter (ANT) (Beltramo et al. 1997 Di Marzo et al. 1994 Fegley et al. 2004 Hillard et al. 1997). The above three proteins and the two cannabinoid receptors have received considerable attention and show great promise as potential targets for the development of novel medications for various conditions, including pain, immunosuppression, peripheral vascular disease, appetite enhancement or suppression, and motor disorders. [Pg.211]

Substitution of the 2-hydroxyethyl group with a phenolic group results in decreased affinity for CBi (Khanolkar et al. 1996). However, N-(o-hydroxy)phenyl-arachidonamide (AM403) was found to be an excellent substrate for FAAH (Lang et al. 1999) while a second phenolic analog, N-(p-hydroxy)phcnylarachidonamide (AM404), was found to be an inhibitor for the anandamide transporter (ANT)... [Pg.228]

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