Summary
The potent dopamine receptor antagonist [3H]-spiroperidol was used to label binding sites in a membrane fraction derived from rabbit mesenteric artery which had characteristics expected for dopamine receptors. The binding was of high affinity with an equilibrium dissociation constant (KD) of 13.1 nM; it was saturable with 110 fmol of [3H]-spiroperidol bound/mg protein at maximal occupancy of the sites. Binding at 37° C was rapid and readily reversible with rate constants of 0.0154 nM−1 min−1 and 0.114 min−1 for forward and reverse reaction, respectively. Dopamine receptor antagonists were about 100–200 times more potent than α-adrenolytic drugs in competing for the [3H]-spiroperidol binding sites and dopamine was much more potent than (−)-noradrenaline, adrenaline, (−)-isoprenaline, clonidine or serotonin. It is concluded that in a membrane fraction of the rabbit mesenteric artery there exist binding sites for [3H]-spiroperidol indistinguishable from dopamine receptors. Thus the present results support the view that in vascular smooth muscle there exist specific dopamine receptors.
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This work was supported by the Deutsche Forschungsgemeinschaft
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Brodde, O.E., Gross, G. [3H]-Spiroperidol labels dopamine receptors in membranes from rabbit mesenteric artery. Naunyn-Schmiedeberg's Arch. Pharmacol. 311, 249–254 (1980). https://doi.org/10.1007/BF00569404
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DOI: https://doi.org/10.1007/BF00569404