Identification of stereospecific [ 3H]spiroperidol binding sites in mammalian lymphocytes

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 (K D1 = 1.9 nM, K D2 = 36.2 nM). Determination of the K D by kinetic studies measuring rate constants for association and dissociation provided K D 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.