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Identification of stereospecific [3H]spiroperidol binding sites in mammalian lymphocytes
Authors:G Le Fur  T Phan  A Uzan
Institution:Pharmindustrie, Groupe PHARMUKA 35, quai du Moulin de Cage, F 92231 Gennevilliers, France
Abstract:Direct binding to intact rat lymphocytes has been shown for the potent dopaminergic antagonist 3H]spiroperidol. The specific binding is saturable with two components (KD1 = 1.9 nM, KD2 = 36.2 nM). Determination of the KD by kinetic studies measuring rate constants for association and dissociation provided KD values similar to those obtained in equilibrium experiments. The specific binding is proportional to cell concentration and temperature dependent with a maximum at 37°C. 3H]spiroperidol binding is stereospecific since (+)butaclamol was more effective than (?)butaclamol. The relative potencies of different antidopaminergic agents in competing for 3H]spiroperidol binding sites parallel their activity in the striatum. Dopaminergic receptors have also been demonstrated in other mammalian lymphocytes (rabbit, dog, human). Lymphocyte dopaminergic receptors could be implicated in lymphocytes mediated immune response.
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