Time course of dopamine1,2 and serotonin2 receptor binding of antipsychotics in vivo
| Autor: | K. Shiba, K. Suzuki, Nariyoshi Yamaguchi, H. Kido, Tomiki Sumiyoshi, Hirofumi Mori, H. Sakamoto, K. Urasaki |
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| Rok vydání: | 1994 |
| Předmět: |
Male
medicine.medical_specialty medicine.drug_class medicine.medical_treatment Clinical Biochemistry Atypical antipsychotic Pharmacology Ligands Toxicology Biochemistry D1 D2 5-HT2 receptors Behavioral Neuroscience Dibenzazepines Dopamine receptor D2 Internal medicine medicine Haloperidol Animals Rats Wistar Antipsychotic Receptor Clozapine Biological Psychiatry Receptors Dopamine D2 Chemistry Receptors Dopamine D1 Dopamine antagonist Rats Neostriatum Endocrinology Receptors Serotonin RMI-81582 Time course study Serotonin In vivo receptor binding Antipsychotic Agents medicine.drug |
| Zdroj: | Pharmacology Biochemistry and Behavior. 49:165-169 |
| ISSN: | 0091-3057 |
| DOI: | 10.1016/0091-3057(94)90471-5 |
| Popis: | 金沢大学疾患モデル総合研究センター An in vivo receptor binding technique was applied to evaluate the affinities of clozapine (20 mg/kg), RMI-81582 (20 mg/kg), and haloperidol (1 mg/kg) for dopamine D1, D2 and serotonin 5-HT2 receptors in rat brain with [3H]-SCH23390, [3H]-YM-09151-2, and [3H]-ketanserin as selective ligands. The time course study of receptor occupancy at 25 to 250 min after intraperitoneal administration of the drugs showed higher 5-HT2 and lower D2 receptor occupancies of clozapine and RMI-81582 than those of haloperidol both in the striatum and frontal cortex. The 5-HT2/D2 ratios of receptor occupancy for clozapine and RMI-81582 were about 6 to 8 times higher than that for haloperidol. Stable occupancies of D1 receptors were observed only with RMI-81582 and clozapine, the former demonstrating the higher occupancy. These findings are in agreement with the previous findings obtained under in vitro conditions and may account for some part of the properties of atypical antipsychotic drugs. © 1994. |
| Databáze: | OpenAIRE |
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