A. Charalambous et al., SYNTHESIS OF (2-[C-11]METHOXY)ROTENONE, A MARKER OF MITOCHONDRIAL COMPLEX-I ACTIVITY, Nuclear medicine and biology, 22(1), 1995, pp. 65-69
Recent studies suggest that defects in the function of the complexes o
f the electron transport chain might be involved in the pathology of n
eurological diseases such as mitochondrial encephalopathies, Parkinson
's, Huntington's and Alzheimer's disease. Rotenone is a potent reversi
ble competitive inhibitor of complex I (NADH-CoQ reductase). To study
the possible involvement of complex I in such diseases, we synthesized
(2-[C-11]methoxy)rotenone by [C-11]alkylation of 2-O-desmethyl roteno
ne methyl enol ether followed by hydrolysis of the enol ether to the k
etone using aqueous trifluoroacetic acid. (2-[C-11]Methoxy)rotenone wa
s purified by high pressure liquid chromatography (silica gel) and was
obtained in 7-10% yields decay corrected to end of bombardment in syn
thesis times typically shorter than 48 min. Radiochemical purities wer
e over 95% and specific activities averaged 1000 Ci/mmol at end of syn
thesis.