Abstract
The present investigation examines WIN 55,212-2 and AM630 at the cloned human cannabinoid CB1 receptor stably expressed in Chinese hamster ovary (CHO) cells. The effect of various concentrations of WIN 55,212-2 and AM630 on basal [35S]GTPgammaS binding to cell membranes was determined. WIN 55,212-2 (100 microM) stimulated basal [35S]GTPgammaS binding 77.9% with an EC50 value of 0.36 microM. Conversely, AM630 (100 microM) inhibited basal [35S]GTPgammaS binding by 20.9% with an EC50 value of 0.90 microM. These results show that WIN 55,212-2 is an agonist and AM630 is an inverse agonist in this system.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Benzoxazines
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CHO Cells
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Cell Membrane / drug effects
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Cell Membrane / metabolism
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Cricetinae
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Guanosine 5'-O-(3-Thiotriphosphate) / metabolism
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Humans
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Indoles / pharmacology*
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Morpholines / pharmacology
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Naphthalenes / pharmacology
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Receptors, Cannabinoid
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Receptors, Drug / antagonists & inhibitors*
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Recombinant Proteins / antagonists & inhibitors
Substances
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Benzoxazines
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Indoles
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Morpholines
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Naphthalenes
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Receptors, Cannabinoid
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Receptors, Drug
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Recombinant Proteins
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Guanosine 5'-O-(3-Thiotriphosphate)
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(3R)-((2,3-dihydro-5-methyl-3-((4-morpholinyl)methyl)pyrrolo-(1,2,3-de)-1,4-benzoxazin-6-yl)(1-naphthalenyl))methanone
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iodopravadoline