Croatica Chemica Acta, Vol. 75 No. 1, 2002.
Original scientific paper
Binding of Dihydroergosine to 5-HT1A Receptors of Human and Rat Brain
Dorotea Mück-Šeler
; Ruđer Bošković Institute, Division of Molecular Medicine, Laboratory for Molecular Neuropharmacology, P.O.B. 180, 10002 Zagreb, Croatia
Danka Peričić
; Ruđer Bošković Institute, Division of Molecular Medicine, Laboratory for Molecular Neuropharmacology, P.O.B. 180, 10002 Zagreb, Croatia
Abstract
Interaction of the ergot alkaloid dihydroergosine with the binding of (3H)8-hydroxy-2-(di-n-propylamino)tetralin (3H8-OH-DPAT), a selective agonist for 5-HT1A binding sites, to hippocampal membra-nes isolated from human and rat brain was studied. Competition binding experiments showed that dihydroergosine is a potent dis-placer of (3H)8-OH-DPAT binding at brain 5-HT1A receptors of both species. Scatchard analysis of (3H)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 (3H)8-OH-DPAT labelled binding sites. Pre-incubation of rat hippocampal membranes for 180 min with dihy-droergosine (2 nmol dm-3) completely prevented the binding of (3H)8-OH-DPAT (2 nmol dm-3). The data suggest that dihydroergo-sine 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.
Keywords
ergot alkaloid; 5-HT<sub>1A</sub> receptors; (<sup>3</sup>H)8-OH-DPAT binding; hippocampus; human brain; rat brain
Hrčak ID:
127499
URI
Publication date:
4.2.2002.
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