Characterization of [3H]ZM 241385 binding in wild-type and adenosine A2A receptor knockout mice.
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.
Kelly
Mary
M
School of Biomedical and Molecular Sciences, University of Surrey, Guildford, Surrey GU2 7XH, UK.
Bailey
Alexis
A
Ledent
Catherine
C
Kitchen
Ian
I
Hourani
Susanna
S
D000818:Animals; D001665:Binding Sites / Q000187:drug effects; D001921:Brain / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D008297:Male; D051379:Mice; D018345:Mice, Knockout; D011485:Protein Binding / Q000502:physiology; D043705:Receptor, Adenosine A2A / Q000172:deficiency* / Q000235:genetics / Q000378:metabolism*; D014227:Triazines / Q000378:metabolism*; D014230:Triazoles / Q000378:metabolism*; D014316:Tritium
D043705:Receptor, Adenosine A2A; D014227:Triazines; D014230:Triazoles; C097270:ZM 241385; D014316:Tritium