Affinity of neuroleptics for D1 receptor of human brain striatum.
Article Details
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Kanba S, Suzuki E, Nomura S, Nakaki T, Yagi G, Asai M, Richelson E
Affinity of neuroleptics for D1 receptor of human brain striatum.
J Psychiatry Neurosci. 1994 Jul;19(4):265-9.
- PubMed ID
- 7918347 [ View in PubMed]
- Abstract
We determined the inhibition-dissociation constant (Ki) of a number of neuroleptics for D1 receptors of normal human brain tissue using [3H]SCH23390 [R-(+)-8-chloro-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3[benzazepine-7- ol]. SCH23390 had the highest affinity with a Ki of 0.76 nM. Among clinically used drugs, propericiazine showed the highest affinity with a Ki of 10 nM. When neuroleptics were classified according to chemical structures, the Ki values were as follows. Phenothiazines ranged from 10 nM to 250 nM. Butyrophenones ranged from 45 nM to 250 nM. Thioxanthenes ranged from 12 nM to 340 nM. Orthopramines were more than 10,000 nM. The Ki values for the binding site of this study were significantly correlated with those reported in studies using animal brain. The possible relationship between D1 receptors and negative symptoms is discussed.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Acepromazine Dopamine D1 receptor Protein Humans YesAntagonistDetails Chlorpromazine Dopamine D1 receptor Protein Humans YesAntagonistDetails Periciazine Dopamine D1 receptor Protein Humans YesAntagonistDetails Pipotiazine Dopamine D1 receptor Protein Humans YesAntagonistDetails Thioproperazine Dopamine D1 receptor Protein Humans UnknownAntagonistDetails Thiothixene Dopamine D1 receptor Protein Humans YesAntagonistDetails