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Differential [(3)H]idazoxan and [(3)H]2-(2-benzofuranyl)-2-imidazoline (2-BFI) binding to imidazoline I(2) receptors in human postmortem frontal cortex

Callado, L F ; Maeztu, A I ; Ballesteros, J ; Gutiérrez, M ; Meana, J J

European journal of pharmacology, 2001-07, Vol.423 (2-3), p.109-114 [Periódico revisado por pares]

Netherlands

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Título:
Differential [(3)H]idazoxan and [(3)H]2-(2-benzofuranyl)-2-imidazoline (2-BFI) binding to imidazoline I(2) receptors in human postmortem frontal cortex
Autor: Callado, L F ; Maeztu, A I ; Ballesteros, J ; Gutiérrez, M ; Meana, J J
Assuntos: Adrenergic alpha-Antagonists - metabolism ; Adrenergic alpha-Antagonists - pharmacology ; Autopsy ; Benzofurans - metabolism ; Benzofurans - pharmacology ; Binding, Competitive - drug effects ; Dose-Response Relationship, Drug ; Frontal Lobe - drug effects ; Frontal Lobe - metabolism ; Humans ; Idazoxan - metabolism ; Idazoxan - pharmacology ; Imidazoles - metabolism ; Imidazoles - pharmacology ; Imidazoline Receptors ; Membranes - drug effects ; Membranes - metabolism ; Radioligand Assay ; Receptors, Drug - metabolism ; Tritium
É parte de: European journal of pharmacology, 2001-07, Vol.423 (2-3), p.109-114
Notas: ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
Descrição: [(3)H]2-(2-benzofuranyl)-2-imidazoline (2-BFI) and [(3)H]idazoxan are the most used tools to characterise imidazoline I(2) receptors. We evaluated the binding of both radioligands to human postmortem frontal cortex membranes. Saturation binding analyses revealed that [(3)H]idazoxan (in the presence of 2 microM efaroxan to avoid radioligand binding to alpha(2)-adrenoceptors and imidazoline I(1) receptors) and [(3)H]2-BFI bound with high affinity to an apparent single population of sites. However, in competition studies whereas [(3)H]idazoxan (10 nM) binding was displaced monophasically by idazoxan and 2-BFI, both drugs displayed biphasic curves for [(3)H]2-BFI (1 nM). The proportion of the low-affinity binding site increased from 17% to 25% when 10 nM [(3)H]2-BFI was displaced by idazoxan. Amiloride inhibited [(3)H]2-BFI (10 nM) binding with low affinity and in a monophasic way. These data indicate that [(3)H]2-BFI recognises in human postmortem brain membranes a second binding site different from the imidazoline I(2) receptors labelled by [(3)H]idazoxan.
Editor: Netherlands
Idioma: Inglês

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Differential [(3)H]idazoxan and [(3)H]2-(2-benzofuranyl)-2-imidazoline (2-BFI) binding to imidazoline I(2) receptors in human postmortem frontal cortex

Callado, L F ; Maeztu, A I ; Ballesteros, J ; Gutiérrez, M ; Meana, J J

Netherlands

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