Mapping adenosine A(1) receptors in the cat brain by positron emission tomography with [(11)C]MPDX.
We evaluated the potential of [(11)C]MPDX as a radioligand for mapping adenosine A(1) receptors in comparison with previously proposed [(11)C]KF15372 in cat brain by PET. Two tracers showed the same brain distribution. Brain uptake of [(11)C]MPDX (Ki = 4.2 nM) was much higher and washed out faster than that of [(11)C]KF15372 (Ki = 3.0 nM), and was blocked by carrier-loading or displaced with an A(1) antagonist. The regional A(1) receptor distribution evaluated with kinetic analysis is consistent with that previously measured in vitro. [(11)C]MPDX PET has a potential for mapping adenosine A(1) receptors in brain.
Shimada
Yuhei
Y
Positron Medical Center, Tokyo Metropolitan Institute of Gerontology, 1-1 Naka-cho, Itabashi-ku, Tokyo 172-0022, Tokyo, Japan.
Ishiwata
Kiichi
K
Kiyosawa
Motohiro
M
Nariai
Tadashi
T
Oda
Keiichi
K
Toyama
Hinako
H
Suzuki
Fumio
F
Ono
Kenichirou
K
Senda
Michio
M
D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism; D002415:Cats; D004232:Diuretics / Q000493:pharmacokinetics*; D011869:Radioligand Assay; D018047:Receptors, Purinergic P1 / Q000378:metabolism*; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed; D019820:Xanthine / Q000493:pharmacokinetics*; D014970:Xanthines / Q000493:pharmacokinetics*
C451639:1-methyl-8-dicyclopropylmethyl-1-methyl-3-propylxanthine; D004232:Diuretics; D018047:Receptors, Purinergic P1; D014970:Xanthines; C067197:8-(dicyclopropylmethyl)-1,3-dipropylxanthine; D019820:Xanthine