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Time Course of Dopamine‐D 2 and Serotonin‐5‐HT 2 Receptor Occupancy Rates by Haloperidol and Clozapine In Vivo
Author(s) -
Sumiyoshi Tomiki,
Kido Hideki,
Sakamoto Hiroshi,
Urasaki Koji,
Suzuki Kimiko,
Yamaguchi Nariyoshi,
Mori Hirofumi,
Shiba Kazuhiro,
Yokogawa Koiçhi,
Ichimura Fujio
Publication year - 1993
Publication title -
psychiatry and clinical neurosciences
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.609
H-Index - 74
eISSN - 1440-1819
pISSN - 1323-1316
DOI - 10.1111/j.1440-1819.1993.tb02041.x
Subject(s) - clozapine , haloperidol , 5 ht receptor , serotonin , occupancy , dopamine receptor d2 , dopamine , pharmacology , chemistry , medicine , schizophrenia (object oriented programming) , receptor , psychiatry , biology , ecology
In vivo occupancy of dopamine‐D 1 , D 2 and serotonin‐5‐HT 2 receptors by haloperidol 10 mg/kg and clozapine 20 mg/kg were studied. Rats were injected intravenously with [ 3 H]‐YM‐09151‐2, [ 3 H]‐SCH23390, or [ 3 H]‐ketanserin 10 min after the administration of the tested drugs. Fifteen to 240 min after the ligand injection, the receptor occupancy rates of the drugs in the striatum and frontal cortex were calculated. Clozapine demonstrated the higher 5‐HT 2 and lower D 2 occupancies in the respective regions. A dose‐response analysis of D 2 and 5‐HT 2 , receptor occupancy by the drugs consolidated the higher 5‐HT 2 binding affinity of clozapine in comparison with haloperidol. The present methodology may serve as an accurate tool to evaluate the peculiarity of various antipsychotics.