Abstract
The baculovirus system has been used to express the rat dopamine D1 receptors in Spodoptera frugiperda (Sf9) cells. A panel of typical antipsychotics including, α-flupenthixol, fluphenazine and thioridizine were found to inhibit dopamine-dependent stimulation of adenylyl cyclase. However, these compounds were also found to inhibit adenylyl cyclase activity in the absence of agonist in Sf9 cells expressing dopamine D1-like receptors. Therefore, these nonselective dopamine receptor compounds displayed negative intrinsic or inverse agonist activity. None of the compounds tested were neutral antagonists.
| Original language | English |
|---|---|
| Pages (from-to) | 73-82 |
| Number of pages | 10 |
| Journal | European Journal of Pharmacology |
| Volume | 420 |
| Issue number | 2-3 |
| DOIs | |
| State | Published - 25 May 2001 |
Keywords
- Adenylyl cyclase stimulation
- Antipsychotic
- Baculovirus expression
- Dopamine D1 receptor
- Dopamine receptor
- Inverse agonist
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Cite this
Martin, M. W., Scott, A. W., Johnston, D. E., Griffin, S., & Luedtke, R. R. (2001). Typical antipsychotics exhibit inverse agonist activity at rat dopamine D1-like receptors expressed in Sf9 cells. European Journal of Pharmacology, 420(2-3), 73-82. https://doi.org/10.1016/S0014-2999(01)00982-7