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Low-affinity conditions for agonists increase the binding of the antagonist [3H]RX821002 to the alpha(2B/C)-adrenoceptor subtypes in human brain and rat kidney

Callado, L F ; Meana, J J

European journal of pharmacology, 1997-07, Vol.332 (1), p.109-112 [Periódico revisado por pares]

Netherlands

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Título:
Low-affinity conditions for agonists increase the binding of the antagonist [3H]RX821002 to the alpha(2B/C)-adrenoceptor subtypes in human brain and rat kidney
Autor: Callado, L F ; Meana, J J
Assuntos: Adrenergic alpha-Antagonists - metabolism ; Adrenergic alpha-Antagonists - pharmacology ; Animals ; Brain - drug effects ; Brain - metabolism ; Brain Chemistry - drug effects ; Guanylyl Imidodiphosphate - pharmacology ; Humans ; Idazoxan - analogs & derivatives ; Idazoxan - metabolism ; Idazoxan - pharmacology ; Kidney - chemistry ; Kidney - drug effects ; Kidney - metabolism ; Male ; Membranes - metabolism ; Rats ; Rats, Sprague-Dawley ; Receptors, Adrenergic, alpha-2 - drug effects ; Receptors, Adrenergic, alpha-2 - metabolism ; Tritium
É parte de: European journal of pharmacology, 1997-07, Vol.332 (1), p.109-112
Notas: ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
Descrição: The mixture of 5'-guanylylimidodiphosphate (Gpp(NH)p)/EDTA/NaCl has been used to delineate low-affinity conditions for agonists binding to G-protein-linked receptors. The effects of this mixture on [3H]RX821002 (2-methoxyidazoxan) binding to alpha2-adrenoceptors were evaluated in different tissues. The density of alpha2-adrenoceptors in the presence of the mixture was 11, 78 and 60% higher in human cortex (predominant alpha2A), human caudate (alpha2A + alpha2C) and rat kidney (alpha2A + alpha2B), respectively, than in its absence. In rat kidney, masking of alpha2B-adrenoceptors by ARC239 (2-[2-[4-(o-methoxyphenyl)-piperazin-1-yl]-ethyl]-4,4-dimethyl-1,3 -(2H,4H)-isoquinolindione) (50 nM) or masking of alpha2A-adrenoceptors by BRL44408 (2-[2H-(1-methyl-1,3-dihydroisoindole)methyl]-4,5-dihydroimidaz ole) (100 nM) demonstrated that the increase was in the alpha2B-adrenoceptor but not in the alpha2A-adrenoceptor subtype.
Editor: Netherlands
Idioma: Inglês

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Low-affinity conditions for agonists increase the binding of the antagonist [3H]RX821002 to the alpha(2B/C)-adrenoceptor subtypes in human brain and rat kidney

Callado, L F ; Meana, J J

Netherlands

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