Abstract |
Dopamine-receptor blockade seems to be a prominent effect of neuroleptics. Blockade of other receptors might, however, contribute to the therapeutic effect. A series of neuroleptics have been tested for affinity to DA D-1 and D-2 receptors, serotonin receptors (S2), alpha- adrenoceptors (alpha 1), histamine receptors (H1), and muscarinic cholinergic receptors. According to the affinity to DA D-1 and D-2 receptors, neuroleptics can be divided into different groups. Thioxanthenes have affinity for both D-1 and D-2 receptors; phenothiazines have affinity for D-2 receptors and considerably lower affinity for D-1 receptors; and butyrophenones, diphenylbutylpiperidines, and benzamides have affinity only for D-2 receptors. Concerning affinity to other receptors the only consistent finding is affinity for S2 receptors. The clinical significance of these findings is speculative. In several behavioral tests the D-1/D-2 classification is also observed, and it is suggested that D-1-receptor activation is responsible for dyskinesia, and that thioxanthenes - due to their D-1 receptor blocking effect-induce less dyskinesia than other neuroleptics.
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Authors | J Hyttel, J J Larsen, A V Christensen, J Arnt |
Journal | Psychopharmacology. Supplementum
(Psychopharmacology Suppl)
Vol. 2
Pg. 9-18
( 1985)
ISSN: 0179-8456 [Print] Germany |
PMID | 2860665
(Publication Type: Journal Article)
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Chemical References |
- Antipsychotic Agents
- Receptors, Dopamine
- Receptors, Dopamine D1
- Receptors, Dopamine D2
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Topics |
- Antipsychotic Agents
(metabolism)
- Binding, Competitive
- Brain
(metabolism)
- Humans
- Kinetics
- Receptors, Dopamine
(metabolism)
- Receptors, Dopamine D1
- Receptors, Dopamine D2
- Schizophrenia
(metabolism)
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