caa a22 4500 46912010X CHVBK 20180323133136.0 cr unu---uuuuu 170328e19920501xx s 000 0 eng 10.1007/BF02244961 doi (NATIONALLICENCE)springer-10.1007/BF02244961 Farde Lars Department of Psychiatry and Psychology, The Karolinska Institute, S-104 01, Stockholm, Sweden aut Selective D1- and D2-dopamine receptor blockade both induces akathisia in humans — a PET study with [11C]SCH 23390 and [11C]raclopride [Elektronische Daten] [Lars Farde] Pharmacological effects were recorded and time course for receptor binding in brain was followed by positron emission tomography after IV injection of the selective D1-dopamine receptor antagonist SCH 23390 in four healthy subjects in doses of 310-810 µg. Akathisia, the syndrome of motor restlessness, appeared after the three highest doses. The akathisia was transient and occurred only when [11C]SCH 23390 binding in the basal ganglia was at a high level with a central D1-dopamine receptor occupancy of 45-59%. The D2-dopamine receptor antagonist [11C]raclopride was injected IV into 20 healthy subjects and 13 schizophrenic patients. Akathisia appeared in 14 healthy subjects and 7 patients and coincided with maximal [11C]raclopride binding in the basal ganglia. The findings for [11C]raclopride and [11C]SCH 23390 are the first demonstration of a relationship between time courses for radioligand binding in the human brain and simultaneously induced pharmacological effects. Springer-Verlag, 1992 Dopamine receptors nationallicence Positron emission tomography nationallicence Akathisia nationallicence SCH 23390 nationallicence Raclopride nationallicence Psychopharmacology Springer-Verlag 107/1(1992-05-01), 23-29 0033-3158 107:1<23 1992 107 213 https://doi.org/10.1007/BF02244961 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/BF02244961 text/html Onlinezugriff via DOI NATIONALLICENCE 100 1- Farde Lars Department of Psychiatry and Psychology, The Karolinska Institute, S-104 01, Stockholm, Sweden aut NATIONALLICENCE 773 0- Psychopharmacology Springer-Verlag 107/1(1992-05-01), 23-29 0033-3158 107:1<23 1992 107 213 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer