Antagonism by neuroleptics of neurotransmitter receptors of normal human brain in vitro.
Article Details
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Richelson E, Nelson A
Antagonism by neuroleptics of neurotransmitter receptors of normal human brain in vitro.
Eur J Pharmacol. 1984 Aug 17;103(3-4):197-204.
- PubMed ID
- 6149136 [ View in PubMed]
- Abstract
Using radioligand binding techniques, we determined the equilibrium dissociation constants (KD's) for a series of neuroleptics at the dopamine (D-2), muscarinic, histamine H1, alpha 1- and alpha 2-adrenergic receptors of normal human brain tissue obtained at autopsy. Seventeen different compounds were studied at the D-2 receptor and 15 compounds at the remaining receptors. At the D-2 receptor of caudate nucleus, spiperone was the most potent compound (KD = 0.16 nM); clozapine the least potent (KD = 180 nM). The KD's for six compounds at the D-2 receptor of nucleus accumbens were not significantly different from their respective KD's in the caudate nucleus. The most potent and least potent compounds at the other receptors were clozapine and molindone at the muscarinic receptor, mesoridazine and molindone at the H1 receptor, spiperone and molindone at the alpha 1-receptor, and clozapine and haloperidol at the alpha 2-receptor, respectively.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Chlorpheniramine Histamine H1 receptor Ki (nM) 15 N/A N/A Details Chlorpromazine Histamine H1 receptor Ki (nM) 9 N/A N/A Details Clozapine Alpha-2A adrenergic receptor Ki (nM) 160 N/A N/A Details Clozapine Histamine H1 receptor Ki (nM) 2.8 N/A N/A Details Clozapine Muscarinic acetylcholine receptor M2 Ki (nM) 12 N/A N/A Details Loxapine Alpha-2A adrenergic receptor Ki (nM) 2400 N/A N/A Details Loxapine Histamine H1 receptor Ki (nM) 4.9 N/A N/A Details Loxapine Muscarinic acetylcholine receptor M2 Ki (nM) 450 N/A N/A Details Promazine Histamine H1 receptor Ki (nM) 2 N/A N/A Details Yohimbine Alpha-2A adrenergic receptor Ki (nM) 2.7 N/A N/A Details Yohimbine Alpha-2A adrenergic receptor Ki (nM) 1.6 N/A N/A Details