Journal of Neurophysiology, Vol 73, Issue 2 907-910, Copyright © 1995 by APS

ARTICLES

Cannabinoid agonists inhibit the activation of 5-HT3 receptors in rat nodose ganglion neurons

P. Fan
Laboratory of Molecular and Cellular Neurobiology, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland 20892, USA.

1. Effects of cannabinoid agonists on the serotonin (5-HT)3 receptor-mediated current were investigated in rat nodose ganglion neurons. Anandamide, Win 55212-2, and CP55940 inhibited the 5-HT-induced current in a concentration dependent manner. IC50 values were 190, 310, and 94 nM for anandamide, Win 55212-2, and CP55940, respectively, and 1.6 microM for the nonpsychoactive enantiomer CP56667. This inhibition was slowly developing, noncompetitive, not dependent on membrane potential, and not affected by adenosine 3',5'-cyclic monophosphate (cAMP) analogues, guanosine-5'-O-(2-thiodiphosphate) (GDP-beta-S), and opioid receptor antagonist naltrexone. These data suggest that 5-HT3 receptor ion-channel is a site acted upon by cannabinoid agonists in the nervous system, and the action of cannabinoid agonists on 5-HT3 receptors may be a possible mechanism for some of the behavioral effects of cannabinoids, such as antiemesis and analgesia.

This article has been cited by other articles:

				W. Xiong, M. Hosoi, B.-N. Koo, and L. Zhang Anandamide Inhibition of 5-HT3A Receptors Varies with Receptor Density and Desensitization Mol. Pharmacol., February 1, 2008; 73(2): 314 - 322. [Abstract] [Full Text] [PDF]

				P. Pacher, S. Batkai, and G. Kunos The Endocannabinoid System as an Emerging Target of Pharmacotherapy Pharmacol. Rev., September 1, 2006; 58(3): 389 - 462. [Abstract] [Full Text] [PDF]

				N. Hejazi, C. Zhou, M. Oz, H. Sun, J. H. Ye, and L. Zhang {Delta}9-Tetrahydrocannabinol and Endogenous Cannabinoid Anandamide Directly Potentiate the Function of Glycine Receptors Mol. Pharmacol., March 1, 2006; 69(3): 991 - 997. [Abstract] [Full Text] [PDF]

				S. A. Moore, G. G. Nomikos, A. K. Dickason-Chesterfield, D. A. Schober, J. M. Schaus, B.-P. Ying, Y.-C. Xu, L. Phebus, R. M. A. Simmons, D. Li, et al. From The Cover: Identification of a high-affinity binding site involved in the transport of endocannabinoids PNAS, December 6, 2005; 102(49): 17852 - 17857. [Abstract] [Full Text] [PDF]

				D. L. Boger, H. Sato, A. E. Lerner, M. P. Hedrick, R. A. Fecik, H. Miyauchi, G. D. Wilkie, B. J. Austin, M. P. Patricelli, and B. F. Cravatt Exceptionally potent inhibitors of fatty acid amide hydrolase: The enzyme responsible for degradation of endogenous oleamide and anandamide PNAS, May 9, 2000; 97(10): 5044 - 5049. [Abstract] [Full Text] [PDF]

				H. Sun, E. A. McCardy, T. K. Machu, and M. P. Blanton Characterization of Interaction of 3,4,5-Trimethoxybenzoic Acid 8-(Diethylamino)octyl Ester with Torpedo californica Nicotinic Acetylcholine Receptor and 5-Hydroxytryptamine3 Receptor J. Pharmacol. Exp. Ther., July 1, 1999; 290(1): 129 - 135. [Abstract] [Full Text]

				D. K. Giang and B. F. Cravatt Molecular characterization of human and mouse fatty acid amide hydrolases PNAS, March 18, 1997; 94(6): 2238 - 2242. [Abstract] [Full Text] [PDF]