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Science 18 December 1992:
Vol. 258. no. 5090, pp. 1946 - 1949
DOI: 10.1126/science.1470919

Articles

Science, Vol 258, Issue 5090, 1946-1949
Copyright © 1992 by American Association for the Advancement of Science


articles

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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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