Abstract
The effects of R(+)-[2,3-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo[1,2,3-de]-1,4- benzoxazin-yl]-(1-napthalenyl)methanone mesylate (WIN 55,212-2) and N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-3-pyrazo le-carboxamide (SR141716A) on guanosine-5'-O-(3-[35S]thio)triphosphate ([35S]GTPgammaS) binding to membranes isolated from human cannabinoid CB1 receptor-transfected Chinese hamster ovary (CHO) cells were examined. WIN 55,212-2 stimulated [35S]GTPgammaS binding 76.3% above basal levels whereas SR141716A produced a 22.3% decrease in basal [35S]GTPgammaS binding. These findings demonstrate that WIN 55,212-2 is an agonist and SR141716A 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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Analgesics / pharmacology*
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Animals
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Benzoxazines
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Binding, Competitive
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CHO Cells / drug effects
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Cricetinae
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Humans
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Morpholines / pharmacology*
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Naphthalenes / pharmacology*
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Piperidines / pharmacology*
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Pyrazoles / pharmacology*
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Receptors, Cannabinoid
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Receptors, Drug / agonists*
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Receptors, Drug / drug effects
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Receptors, Drug / metabolism
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Rimonabant
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Transfection
Substances
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Analgesics
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Benzoxazines
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Morpholines
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Naphthalenes
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Piperidines
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Pyrazoles
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Receptors, Cannabinoid
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Receptors, Drug
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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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Rimonabant