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.
Authors	Shaun Jordan, Ruoyan Chen, Raymond Fernalld, Janelle Johnson, Karen Regardie, Junichi Kambayashi, Yoshihiro Tadori, Hisashi Kitagawa, Tetsuro Kikuchi
Journal	European journal of pharmacology (Eur J Pharmacol) Vol. 540 Issue 1-3 Pg. 53-6 (Jul 01 2006) ISSN: 0014-2999 [Print] Netherlands
PMID	16730695 (Publication Type: Journal Article)
Chemical References	Dopamine Agonists Dopamine Antagonists Receptors, Dopamine D2 Sulfur Radioisotopes Guanosine 5'-O-(3-Thiotriphosphate) Raclopride Ketamine Dizocilpine Maleate Phencyclidine Calcium Dopamine
Topics	Animals Binding, Competitive (drug effects) CHO Cells Calcium (metabolism) Cell Membrane (drug effects, metabolism) Cricetinae Cricetulus Dizocilpine Maleate (pharmacology) Dopamine (pharmacology) Dopamine Agonists (pharmacology) Dopamine Antagonists (pharmacology) Dose-Response Relationship, Drug Gene Expression (genetics) Guanosine 5'-O-(3-Thiotriphosphate) (metabolism) Humans Ketamine (pharmacology) Phencyclidine (pharmacology) Raclopride (pharmacology) Rats Receptors, Dopamine D2 (genetics, metabolism) Sulfur Radioisotopes

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