publication . Article . 2000

Carrier-mediated transport and enzymatic hydrolysis of the endogenous cannabinoid 2-arachidonylglycerol

Beltramo, M; Piomelli, D;
Open Access English
  • Published: 27 Apr 2000
  • Publisher: eScholarship, University of California
  • Country: United States
The human astrocytoma cell line CCF-STTG1 accumulates [3H]2-AG through an Na+- and energy-independent process, with a K(m) of 0.7 ± 0.1 μM. Non- radioactive 2-AG, anandamide or the anandamide transport inhibitor 4- hydroxyphenyl arachidonamide inhibit [3H]2-AG uptake with half-maximal inhibitory concentrations (IC50) of 5.5 ± 1.0 μM, 4.2 ± 0.3 μM and 1.8 ± 0.1 μM, respectively. A variety of lipid transport substrates and inhibitors interfere with neither [3H]2-AG nor [3H]anandamide uptake. These results suggest that 2-AG and anandamide are internalized in astrocytoma cells through a common carrier-mediated mechanism. After incubation with [3H]2-AG, radioactivity...
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