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Nora S. Kula Ross J. Baldessarini John W. Kebabian John L. Neumeyer 《Cellular and molecular neurobiology》1994,14(2):185-191
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. 相似文献
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Dirk T. Witte Jan-Piet Franke Frank J. Bruggeman Durk Dijkstra Rokus A. De Zeeuw 《Chirality》1992,4(6):389-394
In the present study 21 different chiral aminotetralins were used to investigate the mechanism behind their enantiomeric resolution (Rs) on a commercially available high-performance liquid chromatography (HPLC) cellulose tris-3,5-dimethylcarbamate stationary phase. The differences in the chemical structures of the aminotetralins used were never directly located on the chiral carbon. Their chromatographic behavior was studied for two eluent compositions at six different temperatures. Hydrogen bonding and π? π interactions are two possible solute–chiral stationary phase (CSP) interactions. Differences between the enantiomers in their spatial arrangement of positions involved in solute–CSP interactions were the major forces behind enantiomeric separation. Lowering the temperature increased the Rs for the aminotetralins having π-electrons not directly bonded to that part of the molecule where the hydrogen bonding with the CSP is located. Primary amines and secondary amines, with a sufficiently short N-alkyl substituent, showed a decrease of Rs with lower temperatures, all other aminotetralins yielding an increase of Rs with lower temperatures. © 1992 Wiley-Liss, Inc. 相似文献
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