[The inhibition of dopamine D1 and D2 receptors in human putamen by antipsychotic drugs]. 1990

T Kobayashi, and H Shimizu, and M Toru
Department of Psychiatry, Shinshu University School of Medicine, Nagano, Japan.

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.

UI MeSH Term Description Entries
D011699 Putamen The largest and most lateral of the BASAL GANGLIA lying between the lateral medullary lamina of the GLOBUS PALLIDUS and the EXTERNAL CAPSULE. It is part of the neostriatum and forms part of the LENTIFORM NUCLEUS along with the GLOBUS PALLIDUS. Nucleus Putamen,Nucleus Putamens,Putamen, Nucleus,Putamens,Putamens, Nucleus
D011954 Receptors, Dopamine Cell-surface proteins that bind dopamine with high affinity and trigger intracellular changes influencing the behavior of cells. Dopamine Receptors,Dopamine Receptor,Receptor, Dopamine
D002746 Chlorpromazine The prototypical phenothiazine antipsychotic drug. Like the other drugs in this class chlorpromazine's antipsychotic actions are thought to be due to long-term adaptation by the brain to blocking DOPAMINE RECEPTORS. Chlorpromazine has several other actions and therapeutic uses, including as an antiemetic and in the treatment of intractable hiccup. Aminazine,Chlorazine,Chlordelazine,Chlorpromazine Hydrochloride,Contomin,Fenactil,Largactil,Propaphenin,Thorazine,Hydrochloride, Chlorpromazine
D003864 Depression, Chemical The decrease in a measurable parameter of a PHYSIOLOGICAL PROCESS, including cellular, microbial, and plant; immunological, cardiovascular, respiratory, reproductive, urinary, digestive, neural, musculoskeletal, ocular, and skin physiological processes; or METABOLIC PROCESS, including enzymatic and other pharmacological processes, by a drug or other chemical. Chemical Depression,Chemical Depressions,Depressions, Chemical
D005260 Female Females
D006220 Haloperidol A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279) Haldol
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000368 Aged A person 65 years of age or older. For a person older than 79 years, AGED, 80 AND OVER is available. Elderly
D000369 Aged, 80 and over Persons 80 years of age and older. Oldest Old
D001549 Benzamides BENZOIC ACID amides.

Related Publications

T Kobayashi, and H Shimizu, and M Toru
September 1988, Journal of neurochemistry,
T Kobayashi, and H Shimizu, and M Toru
May 1993, The Journal of pharmacology and experimental therapeutics,
T Kobayashi, and H Shimizu, and M Toru
January 1989, Neurochemistry international,
T Kobayashi, and H Shimizu, and M Toru
March 1985, European journal of pharmacology,
T Kobayashi, and H Shimizu, and M Toru
February 1999, European journal of pharmacology,
T Kobayashi, and H Shimizu, and M Toru
August 1988, Neuroscience letters,
T Kobayashi, and H Shimizu, and M Toru
September 2006, Synapse (New York, N.Y.),
T Kobayashi, and H Shimizu, and M Toru
June 1997, British journal of pharmacology,
Copied contents to your clipboard!