[The inhibition of dopamine D1 and D2 receptors in human putamen by antipsychotic drugs].
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.
Kobayashi
T
T
Department of Psychiatry, Shinshu University School of Medicine, Nagano, Japan.
Shimizu
H
H
Toru
M
M
D000368:Aged; D000369:Aged, 80 and over; D014150:Antipsychotic Agents / Q000494:pharmacology*; D001549:Benzamides / Q000494:pharmacology; D001552:Benzazepines / Q000493:pharmacokinetics; D002746:Chlorpromazine / Q000494:pharmacology; D003864:Depression, Chemical; D005260:Female; D006220:Haloperidol / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D011699:Putamen / Q000378:metabolism*; D011954:Receptors, Dopamine / Q000187:drug effects* / Q000378:metabolism; D017447:Receptors, Dopamine D1; D017448:Receptors, Dopamine D2; D013134:Spiperone / Q000493:pharmacokinetics; D013469:Sulpiride / Q000494:pharmacology
D014150:Antipsychotic Agents; D001549:Benzamides; D001552:Benzazepines; D011954:Receptors, Dopamine; D017447:Receptors, Dopamine D1; D017448:Receptors, Dopamine D2; D013134:Spiperone; D013469:Sulpiride; D006220:Haloperidol; C030265:nemonapride; D002746:Chlorpromazine