Stimulating and inhibitory effects of the dopamine "stabilizer" (-)-OSU6162 on dopamine D2 receptor function in vitro
The effect of (-)-OSU6162 on the incorporation of GTPgammaS(35) in the membranes of hD(2l)-transfected CHO cells was investigated. In the absence of dopamine the compound exerted a slight but significant stimulating action, suggesting a weak partial agonism. In the presence of dopamine, low concentr...
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| Veröffentlicht in: | Journal of Neural Transmission 2007-09, Vol.114 (9), p.1143-1146 |
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| container_title | Journal of Neural Transmission |
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| creator | Lahti, R A Tamminga, C A Carlsson, A |
| description | The effect of (-)-OSU6162 on the incorporation of GTPgammaS(35) in the membranes of hD(2l)-transfected CHO cells was investigated. In the absence of dopamine the compound exerted a slight but significant stimulating action, suggesting a weak partial agonism. In the presence of dopamine, low concentrations (10 to 100 nM) enhanced the stimulating action of dopamine. This enhancing effect was reversed by higher concentrations of (-)-OSU6162 in a complex biphasic manner. The dopamine-enhancing action is proposed to be mediated by binding to an allosteric site with high affinity and the inhibitory component by a low-affinity binding to the orthosteric site of the dopamine receptor. |
| doi_str_mv | 10.1007/s00702-007-0784-7 |
| format | Article |
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| ispartof | Journal of Neural Transmission, 2007-09, Vol.114 (9), p.1143-1146 |
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| subjects | Animals CHO Cells Cricetinae Cricetulus Dopamine - physiology Dopamine D2 Receptor Antagonists Dose-Response Relationship, Drug Guanosine 5'-O-(3-Thiotriphosphate) - metabolism Piperidines - pharmacology Receptors, Dopamine D2 - agonists Receptors, Dopamine D2 - physiology |
| title | Stimulating and inhibitory effects of the dopamine "stabilizer" (-)-OSU6162 on dopamine D2 receptor function in vitro |
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