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Binding of dihydroergosine to 5-HT1A receptors of human and rat brain

Muck-Šeler, Dorotea; Peričić, Danka (2002) Binding of dihydroergosine to 5-HT1A receptors of human and rat brain. Croatica Chemica Acta, 75 (1). pp. 235-245. ISSN 0011-1643

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Interaction of the ergot alkaloid dihydroergosine with the binding of (H-3)8-hydroxy-2-(di-n-propylamino)tetralin ((3)H8-OH-DPAT), a selective agonist for 5-HT1A binding sites, to hippocampal membranes isolated from human and rat brain was studied. Competition binding experiments showed that dihydroergosine is a potent displacer of (H-3)8-OH-DPAT binding at brain 5-HT1A receptors of both species. Scatchard analysis of (H-3)8-OH-DPAT binding to rat hippocampal membranes in the presence of dihydroergosine revealed that this ergot compound markedly decreases the number and the affinity of hippocampal (H-3)8-OH-DPAT labelled binding sites. Preincubation of rat hippocampal membranes for 180 min with dihydroergosine (2 nmol dm(-3)) completely prevented the binding of (H-3)8-OH-DPAT (2 nmol dm(-3)). The data suggest that dihydroergosine is approximately as potent a ligand as 8-OH-DPAT for the hippocampal 5-HT1A receptors from human and rat brains, although their kinetics of association and dissociation are apparently different.

Item Type: Article
Uncontrolled Keywords: ergot alkaloid; 5-HT1A receptors; (H-3)8-OH-DPAT binding; hippocampus; human brain; rat brain; antidepressant dihydroergosine; serotonin receptors; messenger-rna; sites; subtypes; radioligand; cortex; 8-hydroxy-2-(di-normal-propylamino)tetralin; selectivity; anxiety
Subjects: NATURAL SCIENCES > Chemistry
Divisions: Division of Molecular Medicine
Project titleProject leaderProject codeProject type
Neurofarmakologija GABA i 5-HT sustavaDanka Peričić00980001MZOS
Neurofarmakologija serotoninskog sustavaDorotea Muck-Šeler0098088MZOS
Neurotransmitori u stresu i regulacija GABA receptora in vitroDanka Peričić0098103MZOS
Depositing User: Dorotea Mueck Šeler
Date Deposited: 19 Nov 2013 11:54

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