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Characterization of [3H]ZM 241385 binding in wild-type and adenosine A2A receptor knockout mice.

par Kelly, Mary;Bailey, Alexis;Ledent, Catherine ;Kitchen, Ian;Hourani, Susanna
Référence European journal of pharmacology, 504, 1-2, page (55-59)
Publication Publié, 2004-11

Article révisé par les pairs

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Résumé :

The binding of the adenosine A(2A) receptor antagonist [3H] 4-(2-[7-amino-2-(2-furyl)[1,2,4]-triazolo[2,3-a][1,3,5]triazin-5-ylamino]ethyl)phenol ([3H]ZM 241385) to mouse brain and spinal cord was investigated. In brain homogenates, single-site binding was observed with a Bmax of 299+/-28 fmol mg(-1) protein and a Kd of 0.75+/-0.08 nM. In autoradiographic studies, there was a high density of specific binding of [3H]ZM 241385 in the striatum, with a very low density in the cortex and no binding elsewhere in the brain or in the spinal cord. All specific binding of [3H]ZM 241385 was lost in genetically modified mice lacking the adenosine A(2A) receptor, confirming the selectivity of this radioligand.