Abstract

The binding of [ 3H](+)-7-hydroxy-2-( N,N-di- n-propylamino)tetralin ([ 3H]7-OH-DPAT) to dopamine D 2 and D 3 receptors expressed in Chinese hamster ovary (CHO) cells was investigated and compared with [ 3H]methylspiperone. [ 3H]7-OH-DPAT labeled the D 3 receptor in the CHO cells in a guanine nucleotide-insensitive fashion and exhibited a K d of about 0.5 nM. In the presence of MgCl 2. [ 3H]7-OH-DPAT was also found to label the D 2 receptor in CHO cells with high affinity (3.6 nM). The binding of [ 3H]7-OH-DPAT to the D 2 receptor was sensitive to guanine nucleotides suggesting occupancy of a high affinity G protein-coupled state of the receptor. These results suggest that caution should be exercised when using [ 3H]7-OH-DPAT to label the dopamine D 3 receptor in brain tissues.

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