Non-competitive interaction between raclopride and spiperone on human D-receptors in intact Chinese hamster ovary cells

Fundamental & Clinical Pharmacology
Ann PackeuGeorges Vauquelin


We recently investigated the binding properties of the antagonists [(3)H]-raclopride and [(3)H]-spiperone to intact Chinese hamster ovary cells expressing recombinant human D(2long)-dopamine receptors (CHO-D(2L) cells). Compared with saturation binding with [(3)H]-raclopride, raclopride reduced [(3)H]-spiperone binding with to low potency in competition binding experiments. The present findings illustrate the ability of spiperone to inhibit [(3)H]-raclopride binding non-competitively. While raclopride only decreases the apparent K(D) of [(3)H]-raclopride in saturation binding experiments, spiperone only decreases the number of sites to which [(3)H]-raclopride binds with high affinity. Also, while the IC(50) of raclopride depends on the concentration of [(3)H]-raclopride in competition experiments, this is not the case for spiperone. Kinetic studies reveal that the binding of raclopride at its high affinity sites does not affect the association of subsequently added [(3)H]-spiperone nor the rebinding of freshly dissociated [(3)H]-spiperone to the same or surrounding receptors. Yet, spiperone does not affect the dissociation rate of [(3)H]-raclopride and raclopride does not affect the (genuine) dissociation rate of [(3)H]-spipero...Continue Reading


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