Summary
1. Our aim was to test the hypothesis that selectivity for D3 dopamine (DA) receptors may contribute to limbic anti-DA selectivity ofS-(+)-aporphine DA partial agonists.
2. Affinity was tested with3H-emonapride, using human D3 receptors in mouse fibroblasts and D2 receptors in rat striatal tissue.
3. D3 receptors showed a picomolar affinity for3H-emonapride, Na+ dependence, and reversible saturability, as well as stereoselectivity. Confirmatory or novel D3/D2 pharmacologic selectivity was found with several benzamides, thioxanthenes, buspirone, GBR-12909, and DA agonists including hydroxyaminotetralins [ADTN, (+)-7-OH-DPAT, (−)-PPHT and its fluorescein derivative], (−)-N-propylnorapomorphine, (−)-3-PPP, (−)-quinpirole, and SDZ-205-502, but neither aminoergoline nor (+)-aporphine partial agonists.
4. The results extend pharmacologic characterization of D3-transfected cell membranes but fail to account for the high limbic anti-DA selectivity ofS-(+)-aporphines.
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Kula, N.S., Baldessarini, R.J., Kebabian, J.W. et al. S-(+)-aporphines are not selective for human D3 dopamine receptors. Cell Mol Neurobiol 14, 185–191 (1994). https://doi.org/10.1007/BF02090784
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DOI: https://doi.org/10.1007/BF02090784