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Science 18 December 1992: Vol. 258. no. 5090, pp. 1946 - 1949 DOI: 10.1126/science.1470919
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Articles
Science, Vol 258, Issue 5090, 1946-1949
Copyright © 1992 by American Association for the Advancement of Science
Isolation and structure of a brain constituent that binds to the cannabinoid receptor
WA Devane,
L Hanus,
A Breuer,
RG Pertwee,
LA Stevenson,
G Griffin,
D Gibson,
A Mandelbaum,
A Etinger,
and
R Mechoulam
Department of Natural Products, Medical Faculty, Hebrew University, Jerusalem, Israel.
Arachidonylethanolamide, an arachidonic acid derivative in porcine brain, was identified in a screen for endogenous ligands for the cannabinoid receptor. The structure of this compound, which has been named "anandamide," was determined by mass spectrometry and nuclear magnetic resonance spectroscopy and was confirmed by synthesis. Anandamide inhibited the specific binding of a radiolabeled cannabinoid probe to synaptosomal membranes in a manner typical of competitive ligands and produced a concentration-dependent inhibition of the electrically evoked twitch response to the mouse vas deferens, a characteristic effect of psychotropic cannabinoids. These properties suggest that anandamide may function as a natural ligand for the cannabinoid receptor.
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- Fatty Acid Amide Hydrolase Determines Anandamide-induced Cell Death in the Liver.
- S. V. Siegmund, E. Seki, Y. Osawa, H. Uchinami, B. F. Cravatt, and R. F. Schwabe (2006)
J. Biol. Chem.
281, 10431-10438
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- Anandamide Uptake Is Consistent with Rate-limited Diffusion and Is Regulated by the Degree of Its Hydrolysis by Fatty Acid Amide Hydrolase.
- M. Kaczocha, A. Hermann, S. T. Glaser, I. N. Bojesen, and D. G. Deutsch (2006)
J. Biol. Chem.
281, 9066-9075
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- Further Characterization of the Time-Dependent Vascular Effects of {Delta}9-Tetrahydrocannabinol.
- S. E. O'Sullivan, D. A. Kendall, and M. D. Randall (2006)
J. Pharmacol. Exp. Ther.
317, 428-438
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- Effect of an unstirred layer on the membrane permeability of anandamide.
- I. N. Bojesen and H. S. Hansen (2006)
J. Lipid Res.
47, 561-570
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- Elevation of Endocannabinoid Levels in the Ventrolateral Periaqueductal Grey through Inhibition of Fatty Acid Amide Hydrolase Affects Descending Nociceptive Pathways via Both Cannabinoid Receptor Type 1 and Transient Receptor Potential Vanilloid Type-1 Receptors.
- S. Maione, T. Bisogno, V. de Novellis, E. Palazzo, L. Cristino, M. Valenti, S. Petrosino, V. Guglielmotti, F. Rossi, and V. D. Marzo (2006)
J. Pharmacol. Exp. Ther.
316, 969-982
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- Ex Vivo Imaging of Fatty Acid Amide Hydrolase Activity and Its Inhibition in the Mouse Brain.
- S. T. Glaser, S. J. Gatley, and A. N. Gifford (2006)
J. Pharmacol. Exp. Ther.
316, 1088-1097
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- Phosphorylation-Dependent Desensitization by Anandamide of Vanilloid Receptor-1 (TRPV1) Function in Rat Skeletal Muscle Arterioles and in Chinese Hamster Ovary Cells Expressing TRPV1.
- E. Lizanecz, Z. Bagi, E. T. Pasztor, Z. Papp, I. Edes, N. Kedei, P. M. Blumberg, and A. Toth (2006)
Mol. Pharmacol.
69, 1015-1023
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- N-arachidonoyl L-serine, an endocannabinoid-like brain constituent with vasodilatory properties.
- G. Milman, Y. Maor, S. Abu-Lafi, M. Horowitz, R. Gallily, S. Batkai, F.-M. Mo, L. Offertaler, P. Pacher, G. Kunos, et al. (2006)
PNAS
103, 2428-2433
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- The Emerging Role of the Endocannabinoid System in Endocrine Regulation and Energy Balance.
- U. Pagotto, G. Marsicano, D. Cota, B. Lutz, and R. Pasquali (2006)
Endocr. Rev.
27, 73-100
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- Cannabinoid Analgesia as a Potential New Therapeutic Option in the Treatment of Chronic Pain.
- T. L Burns and J. R Ineck (2006)
Ann. Pharmacother.
40, 251-260
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