Neuroleptic binding to human brain receptors: relation to clinical effects.

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Richelson E

Neuroleptic binding to human brain receptors: relation to clinical effects.

Ann N Y Acad Sci. 1988;537:435-42.

PubMed ID

2904784 [ View in PubMed

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Abstract

Table 2 summarizes the potential clinical consequences of neurotransmitter receptor blockade by neuroleptics. These pharmacological effects of neuroleptics at receptors in brain and elsewhere in the body are likely responsible for therapeutic and certain adverse effects as well as some drug-drug interactions. Data presented here should allow the physician a rational basis for selecting neuroleptics to minimize these unwanted effects in patients.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Chlorpromazine	5-hydroxytryptamine receptor 2C	Ki (nM)	1.4	N/A	N/A	Details
Chlorpromazine	Histamine H1 receptor	Ki (nM)	9.09	N/A	N/A	Details
Clozapine	5-hydroxytryptamine receptor 2C	Ki (nM)	1.58	N/A	N/A	Details
Clozapine	Alpha-2A adrenergic receptor	Ki (nM)	161.29	N/A	N/A	Details
Clozapine	Histamine H1 receptor	Ki (nM)	2.77	N/A	N/A	Details
Clozapine	Muscarinic acetylcholine receptor M2	Ki (nM)	12.04	N/A	N/A	Details
Diphenhydramine	Histamine H1 receptor	Ki (nM)	14.08	N/A	N/A	Details
Fluphenazine	5-hydroxytryptamine receptor 2C	Ki (nM)	188.67	N/A	N/A	Details
Loxapine	5-hydroxytryptamine receptor 2C	Ki (nM)	1.69	N/A	N/A	Details
Loxapine	Alpha-2A adrenergic receptor	Ki (nM)	2380.95	N/A	N/A	Details
Loxapine	Histamine H1 receptor	Ki (nM)	5	N/A	N/A	Details
Loxapine	Muscarinic acetylcholine receptor M2	Ki (nM)	454.54	N/A	N/A	Details
Methysergide	5-hydroxytryptamine receptor 2C	Ki (nM)	6.66	N/A	N/A	Details
Promazine	5-hydroxytryptamine receptor 2C	Ki (nM)	15.87	N/A	N/A	Details
Promazine	Histamine H1 receptor	Ki (nM)	2	N/A	N/A	Details