(-)-Penbutolol as a blocker of central 5-HT1A receptor-mediated responses.

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Hjorth S

(-)-Penbutolol as a blocker of central 5-HT1A receptor-mediated responses.

Eur J Pharmacol. 1992 Nov 3;222(1):121-7.

PubMed ID

1468487 [ View in PubMed

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Abstract

Brain 5-HT1A and 5-HT1B receptors are important targets for drug-induced modulation of 5-HT function in vivo. However, very few compounds are available that are effective antagonists at 5-HT1 receptors, thus hampering the progress of fundamental as well as clinical research in this area. The present study assessed the usefulness of the beta-adrenolytic agent (-)-penbutolol (and its (+)-counterpart) as a 5-HT1A receptor-blocking agent. The compound was found to counteract, in a stereospecific fashion, not only the behavioural and hypothermic but also the in vivo 5-HT synthesis/turnover-reducing effects of the specific 5-HT1A receptor agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT). These findings indicate that (-)-penbutolol is an antagonist at both postsynaptic receptors and somatodendritic autoreceptors of the 5-HT1A subtype. Thus, (-)-penbutolol represents a useful addition to the array of pharmacological tools available for the study of central 5-HT1 receptor-mediated functions.

DrugBank Data that Cites this Article

Drugs

Penbutolol

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Penbutolol	5-hydroxytryptamine receptor 1A	Protein	Humans	Yes	Antagonist	Details