Brain neurotransmitter receptor-binding characteristics in rats after oral administration of haloperidol, risperidone and olanzapine.
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Uchida S, Kato Y, Hirano K, Kagawa Y, Yamada S
Brain neurotransmitter receptor-binding characteristics in rats after oral administration of haloperidol, risperidone and olanzapine.
Life Sci. 2007 Apr 3;80(17):1635-40. Epub 2007 Jan 27.
- PubMed ID
- 17316700 [ View in PubMed]
- Abstract
The present study was conducted to characterize the binding of neurotransmitter receptors (dopamine D(2), serotonin 5-HT(2), histamine H(1), adrenaline alpha(1) and muscarine M(l) receptors) in the rat's brain after the oral administration of haloperidol, risperidone, and olanzapine. Haloperidol at 1 and 3 mg/kg displayed significant activity to bind the D(2) receptor (increase in the Kd value for [(3)H]raclopride binding) in the corpus striatum with little change in the activity toward the 5-HT(2) receptor (binding parameters for [(3)H]ketanserin). In contrast, risperidone (0.1-3 mg/kg) showed roughly 30 times more affinity for the 5-HT(2) receptor than D(2) receptor. Also, olanzapine (1-10 mg/kg) was most active toward the H(1) receptor in the cerebral cortex, corpus striatum, and hippocampus, was less active in binding 5-HT(2) and D(2) receptors, and showed the least affinity for alpha(1) and M(1) receptors. In conclusion, haloperidol and risperidone administered orally selectively bind D(2) and 5-HT(2) receptors, respectively, in the rat brain, while olanzapine binds H(1), 5-HT(2), and D(2) receptors more than alpha(1) and M(1) receptors.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Haloperidol Dopamine D2 receptor Protein Humans YesAntagonistDetails Olanzapine 5-hydroxytryptamine receptor 2A Protein Humans YesAntagonistDetails Olanzapine Alpha-1B adrenergic receptor Protein Humans UnknownAntagonistDetails Olanzapine Dopamine D2 receptor Protein Humans YesAntagonistDetails Olanzapine Histamine H1 receptor Protein Humans UnknownAntagonistDetails Olanzapine Muscarinic acetylcholine receptor M1 Protein Humans UnknownAntagonistDetails