Labeling of histamine H1-receptors in vivo: a compartment model analysis and positron emission tomographic imaging.
Binding of [3H]-pyrilamine to guinea-pig brain in vivo was studied and analyzed kinetically on the basis of a four-compartment model to establish the method of analysis for the in vivo binding. The pharmacological properties of the [3H]-pyrilamine binding in vivo were similar to those of the in vitro binding to brain homogenate. The distribution of histamine H1-receptors in dog brain, which was obtained by positron emission tomography (PET) with [11C]-pyrilamine or doxepin as a tracer, was in good correlation to that obtained by the in vitro binding method. We finally applied this in vivo binding method to a living healthy human to reveal the distribution of H1-receptor in the brain.
Yanai
K
K
Department of Pharmacology I, School of Medicine, Tohoku University, Sendai, Japan.
Watanabe
T
T
Itoh
M
M
Hatazawa
J
J
Iwata
R
R
Ido
T
T
D000818:Animals; D001345:Autoradiography; D001921:Brain / Q000378:metabolism*; D004285:Dogs; D006168:Guinea Pigs; D006801:Humans; D007700:Kinetics; D008297:Male; D008875:Middle Aged; D011738:Pyrilamine / Q000378:metabolism*; D011970:Receptors, Histamine H2 / Q000378:metabolism*; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed; D014316:Tritium
D011970:Receptors, Histamine H2; D014316:Tritium; D011738:Pyrilamine