In vivo characterization of radioiodinated 2-(4-phenylpiperidino)cyclohexanol (vesamicol) analogs: potential radioligand for mapping presynaptic cholinergic neurons.
Iodovesamicol analogs, radioiodinated at the ortho (1), meta(2) and para(3) positions of the 4-phenylpiperidine moiety, were evaluated as potential presynaptic cholinergic neuron mapping agents. Significant accumulation of m-[125I]iodovesamicol (mIV(2)) (about 3% of the injected dose) was noted in the rat brain with prolonged retention times. The accumulation of mIV(2) in the rat brain was decreased by 67% by 5 min pre-injection of dl-vesamicol(1 mumol/kg). Pre-injection of (+)-3-(3-hydroxyphenyl)-N-(1-propyl)piperdine[(+)-3-PPP](0.75 mumol/kg) did not markedly decrease the levels of radiotracers (oIV(1) and mIV(2)) in the rat brain. These results suggest that radioidinated m-iodovesamicol (mIV(2)) is suitable for use in presynaptic cholinergic neuron mapping.
Shiba
K
K
Radiosotope Center, School of Medicine, Kanazawa University, Japan.
Mori
H
H
Matsuda
H
H
Tsuji
S
S
Tonami
N
N
Hisada
K
K
D000818:Animals; D001345:Autoradiography / Q000379:methods; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism*; D007457:Iodine Radioisotopes / Q000378:metabolism; D007700:Kinetics; D008297:Male; D009467:Neuromuscular Depolarizing Agents / Q000378:metabolism* / Q000493:pharmacokinetics; D010880:Piperidines / Q000138:chemical synthesis / Q000378:metabolism* / Q000493:pharmacokinetics; D011869:Radioligand Assay; D011877:Radionuclide Imaging; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship; D013997:Time Factors; D014018:Tissue Distribution
D007457:Iodine Radioisotopes; D009467:Neuromuscular Depolarizing Agents; D010880:Piperidines; C006189:vesamicol