Yakubutsu, seishin, kodo = Japanese journal of psychopharmacology · 1990
[The inhibition of dopamine D1 and D2 receptors in human putamen by antipsychotic drugs].
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Kobayashi T, Shimizu H, Toru M
Аннотация
The inhibition of 3H-SCH 23390 (D1), 3H-spiperone (D2), and 3H-YM-09151 (D2) binding to human putamen membranes by four antipsychotic drugs was studied. Two substituted benzamides, (-)-sulpiride and YM-09151, weakly inhibited specific 3H-SCH 23390 binding to D1 receptor sites. The inhibition of 3H-SCH 23390 binding by haloperidol and chlorpromazine was also weak in the 10(-8)-10(-6) M range. All four drugs potently inhibited 3H-spiperone binding, with the following rank order of potency: haloperidol greater than YM-09151 greater than (-)-sulpiride greater than chlorpromazine. 3H-YM-09151 binding was potently displaced by YM-09151 (10(-9) M) and weakly displaced by (-)-sulpiride (10(-7) M). The potency of inhibition by haloperidol and chlorpromazine was in the 10(-8) M order.