In vitro biochemical evidence that the psychotomimetics phencyclidine, ketamine and dizocilpine (MK-801) are inactive at cloned human and rat dopamine D2 receptors
- PMID:16730695
- DOI: 10.1016/j.ejphar.2006.04.026
In vitro biochemical evidence that the psychotomimetics phencyclidine, ketamine and dizocilpine (MK-801) are inactive at cloned human and rat dopamine D2 receptors
Abstract
Dopamine potently increased calcium mobilization in Chinese hamster ovary cells expressing human dopamine D2Long receptors (CHO-D2L cells), and increased guanosine-5'-O-(3-[35S]thio)-triphosphate binding to CHO-D2L cell and rat striatal membranes. These effects of dopamine were blocked by the dopamine D2 receptor antagonist (-)raclopride. In contrast to the findings of a recent controversial study, phencyclidine, ketamine and dizocilpine (MK-801) lacked dopamine D2 receptor full agonist, partial agonist and antagonist activity in these assays, suggesting their psychotomimetic effects, and activity in rodent models of schizophrenia, are associated with N-methyl-d-aspartate receptor blockade rather than a direct interaction with dopamine D2 receptors.
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