publication . Article . 1997

Functional role of high-affinity anandamide transport, as revealed by selective inhibition

Beltramo, M; Stella, N; Calignano, A; Lin, SY; Makriyannis, A; Piomelli, D;
Open Access English
  • Published: 22 Aug 1997
  • Publisher: eScholarship, University of California
  • Country: United States
Anandamide, an endogenous ligand for central cannabinoid receptors, is released from neurons on depolarization and rapidly inactivated. Anandamide inactivation is not completely understood, but it may occur by transport into cells or by enzymatic hydrolysis. The compound N-(4- hydroxyphenyl)arachidonylamide (AM404) was shown to inhibit high-affinity anandamide accumulation in rat neurons and astrocytes in vitro, an indication that this accumulation resulted from carrier-mediated transport. Although AM404 did not activate cannabinoid receptors or inhibit anandamide hydrolysis, it enhanced receptor-mediated anandamide responses in vitro and in vivo. The data indic...
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