We found a match
Your institution may have access to this item. Find your institution then sign in to continue.
- Title
Functional role of high-affinity anandamide transport, as revealed by selective inhibition.
- Authors
Beltramo, M; Stella, N; Calignano, A; Lin, S Y; Makriyannis, A; Piomelli, D
- Abstract
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 indicate that carrier-mediated transport may be essential for termination of the biological effects of anandamide, and may represent a potential drug target.
- Publication
Science (New York, N.Y.), 1997, Vol 277, Issue 5329, p1094
- ISSN
0036-8075
- Publication type
Journal Article
- DOI
10.1126/science.277.5329.1094