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Saturation of striatal D2 dopamine receptors by clozapine
| Content Provider | Scilit |
|---|---|
| Author | Nyberg, Svante Chou, Yuan-Hwa Halldin, Christer |
| Copyright Year | 2002 |
| Description | Positron emission tomography (PET) studies have demonstrated low striatal $D_{2}$ dopamine receptor occupancy in clozapine-treated schizophrenic patients. The aim of this pilot study was to explore if this low receptor occupancy indeed represents partial saturability of striatal $D_{2}$ dopamine receptors by clozapine. Three anaesthetized Cynomolgus monkeys were examined during one day with PET and $[^{11}$C]raclopride at baseline and after intravenous injections of clozapine 1.5 mg/kg followed by 18.5 mg/kg. The estimated corresponding human oral doses were approx. 210 mg/d and 2800 mg/d. $D_{2}$ dopamine receptor occupancy was calculated using an equilibrium-ratio analysis and ranged from 54 to 58% after 1ยท5 mg/kg and 87 to 89% after the total dose 20 mg/kg. The calculated maximal occupancy was 93%. We conclude that PET-measured $D_{2}$ dopamine receptor occupancy by clozapine can be described using a model based on the law of mass action, previously validated for conventional antipsychotics. Therefore, sufficiently high doses of clozapine are expected to produce complete striatal $D_{2}$ dopamine receptor occupancy. The findings further support our previous findings of low $D_{2}$ dopamine receptor occupancy in patients treated with standard doses of clozapine. |
| Related Links | https://academic.oup.com/ijnp/article-pdf/5/1/11/2046777/5-1-11.pdf |
| Ending Page | 16 |
| Page Count | 6 |
| Starting Page | 11 |
| DOI | 10.1017/S1461145701002693 |
| Journal | International Journal of Neuropsychopharmacology |
| Issue Number | 01 |
| Volume Number | 5 |
| Language | English |
| Publisher | Cambridge University Press (CUP) |
| Publisher Date | 2002-03-01 |
| Access Restriction | Open |
| Subject Keyword | International Journal of Neuropsychopharmacology Striatal D2 Dopamine Receptor Occupancy D2 Dopamine Receptor |
| Content Type | Text |
| Resource Type | Article |
