Evaluation of [125I]7 alpha-O-iodoallyl diprenophine as a new potential SPECT opioid receptor imaging agent.
A new iodinated diprenorphine analog, [125I]7 alpha-O-iodoallyl diprenorphine ([125I]7 alpha-O-IA-DPN), was prepared by iododestannylation and characterized. As an opioid antagonist, this agent showed very high affinity (Ki = 0.4 +/- 0.2 nM) and 63% of specific binding by in vitro and in vivo binding studies. Inhibition curves indicated that this tracer labeled with the same affinities to three opioid receptors (mu = delta = kappa). The findings demonstrate that this proposed compound appears to be potential radioprobe for future study of opioid receptors by in vivo SPECT.
Wang
R F
RF
Department of Nuclear Medicine, First Hospital, Beijing Medical University, People's Republic of China.
Tafani
J A
JA
Francés
B
B
Bergon
M
M
Coulais
Y
Y
Zajac
J M
JM
Guiraud
R
R
D000818:Animals; D001921:Brain / Q000378:metabolism; D004174:Diprenorphine / Q000031:analogs & derivatives; D007457:Iodine Radioisotopes; D008297:Male; D051379:Mice; D009292:Narcotic Antagonists; D051381:Rats; D017208:Rats, Wistar; D011957:Receptors, Opioid / Q000032:analysis*; D014018:Tissue Distribution; D015899:Tomography, Emission-Computed, Single-Photon
D007457:Iodine Radioisotopes; D009292:Narcotic Antagonists; D011957:Receptors, Opioid; D004174:Diprenorphine