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.