Photoaffinity labeling of D-2 dopamine binding subunits from rat striatum, anterior pituitary and olfactory bulb with a new probe, [3H]azidosulpride |
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| Authors: | K Redouane P Sokoloff J C Schwartz P Hamdi A Mann C G Wermuth J Roy J L Morgat |
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| Affiliation: | 1. Unité 109 de Neurobiologie, Centre Paul Broca de l''ISERM, 2 ter rue d''Alésia, 75014 Paris, France;1. Centre de Neurochimie, ERA 393 du CNRS, 5 rue Blaise Pascal, 67000 Strasbourg, France;7. Service de Biochimie, Département de Biologie, Centre d''Etudes Nucléaires de Saclay, 91191 Gif sur Yvette, France;1. Lilly Research Laboratories, Eli Lilly & Co., Lilly Corporate Center, Indianapolis, IN 46285, USA;2. Lilly Research Laboratories, Eli Lilly & Co., Erl Wood Manor, United Kingdom;3. Shanghai ChemPartner, Pudong, Shanghai 201203, China;1. Department of Psychiatry and Behavioral Sciences, Northwestern Feinberg School of Medicine, Chicago, IL, 60611, USA;2. Discovery Chemistry, Lilly Research Laboratories, Eli Lilly & Co., Lilly Corporate Center, Indianapolis, IN, 46285, USA;3. Neuroscience Discovery, Lilly Research Laboratories, Eli Lilly & Co., Lilly Corporate Center, Indianapolis, IN, 46285, USA;1. Department of Psychiatry and Behavioral Sciences, Northwestern Feinberg School of Medicine, Chicago, IL 60611, USA;2. Department of Chemistry, Northwestern University, 2145 Sheridan Road, Evanston, IL 60208, USA;3. Department of Pharmacology, Northwestern Feinberg School of Medicine, Chicago, IL 60611, USA |
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| Abstract: | A novel photoaffinity probe [3H] azidosulpride has been developed for biochemical studies of D-2 dopamine receptors. This ligand binds to the receptors with high affinity (Kd = 3.1 +/- 0.2 nM) and, upon photoactivation, about 20% of the radioactivity bound to membranes becomes covalently incorporated. More than 90% of this irreversible binding is protectable by dopaminergic agents including D-2 selective compounds, whereas D-1 selective and non-dopaminergic compounds are ineffective. Analysis by sodium dodecylsulfate polyacrylamide gel electrophoresis reveals a single band at Mr = 85 kDa for labeled receptors in striatum, anterior pituitary or olfactory bulb, where pharmacologically distinct binding sites have been previously detected. |
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