In vitro biochemical evidence that the psychotomimetics phencyclidine, ketamine and dizocilpine (MK-801) are inactive at cloned human and rat dopamine D2 receptors
| Autor: | Tetsuro Kikuchi, Shaun Jordan, Junichi Kambayashi, Raymond Fernalld, Karen Regardie, Hisashi Kitagawa, Janelle L. Johnson, Yoshihiro Tadori, Ruoyan Chen |
|---|---|
| Rok vydání: | 2006 |
| Předmět: |
medicine.medical_specialty
Dopamine Gene Expression Phencyclidine CHO Cells Pharmacology Sulfur Radioisotopes Binding Competitive Dopamine receptor D1 Cricetulus Dopamine receptor D3 Dopamine receptor D2 Internal medicine Cricetinae medicine Animals Humans Raclopride Dose-Response Relationship Drug Chemistry Receptors Dopamine D2 Dopaminergic Cell Membrane Rats Dizocilpine Endocrinology Dopamine receptor Guanosine 5'-O-(3-Thiotriphosphate) Dopamine Agonists Dopamine Antagonists Calcium Ketamine Dizocilpine Maleate Endogenous agonist medicine.drug |
| Zdroj: | European journal of pharmacology. 540(1-3) |
| ISSN: | 0014-2999 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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