Antagonism by neuroleptics of serotonin 5-HT1A and 5-HT2 receptors of normal human brain in vitro.

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Wander TJ, Nelson A, Okazaki H, Richelson E

Antagonism by neuroleptics of serotonin 5-HT1A and 5-HT2 receptors of normal human brain in vitro.

Eur J Pharmacol. 1987 Nov 10;143(2):279-82.

PubMed ID

2891550 [ View in PubMed

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Abstract

Using radioligand binding techniques and human frontal cortex, we determined the equilibrium dissociation constants (KDs) of 17 neuroleptics at the serotonin 5-HT1A and serotonin 5-HT2 receptors with [3H]WB4101 and [3H]ketanserin, respectively. At the serotonin 5-HT1A receptor, the most and least potent neuroleptics were chlorprothixene (KD = 230 nM) and fluphenazine (KD = 40 microM), respectively. At the serotonin 5-HT2 receptor, the most and least potent neuroleptics were spiperone (KD = 0.38 nM) and molindone, (KD = 5 microM), respectively.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Chlorprothixene	5-hydroxytryptamine receptor 2A	Protein	Humans	Yes	Antagonist	Details