Technetium-99m-MRP20, a potential brain perfusion agent: in vivo biodistribution and SPECT studies in non-primate animals.
MRP20 (N-(2(1H pyrolylmethyl]N'-(4-pentene-3-one-2] ethane-1,2-diamine) complexes with technetium-99m, yielding a neutral, lipophilic species. This compound has been characterized as [TcO(MRP20)]. Biologic investigation of [99mTc][TcO(MRP20)] in female rats showed 2.35% ID in the brain 30 min p.i. with no significant wash-out over 3 hr. A single-photon emission computed tomography (SPECT) study in a dog demonstrated rapid tracer uptake in the brain, reaching a maximum within 1 min, with 2.24% i.d. 15 min p.i., decreasing to 1.7% after 4 hr. The complex undergoes hydrolysis in vitro forming a cationic species. This is possibly the trapping mechanism in the brain in vivo. The main excretory route of [99mTc][TcO(MRP20)] is via the hepatobiliary tract. There is evidence of some "in vivo" cell labeling and soft-tissue uptake.
Morgan
G F
GF
R/D Imaging, Medgenix Group S.A., Fleurus, Belgium.
Deblaton
M
M
Clemens
P
P
Van Den Broeck
P
P
Bossuyt
A
A
Thornback
J R
JR
D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism; D003959:Diamines / Q000493:pharmacokinetics*; D004285:Dogs; D005260:Female; D015609:Organotechnetium Compounds / Q000493:pharmacokinetics*; D011758:Pyrroles / Q000493:pharmacokinetics*; D051381:Rats; D014018:Tissue Distribution; D015899:Tomography, Emission-Computed, Single-Photon
D003959:Diamines; D015609:Organotechnetium Compounds; D011758:Pyrroles; C067798:technetium Tc 99m-(N-(2-(1H)-pyrrolylmethyl))-N'-(4-pentene-3-one)ethane-1,2-diamine