Z-(R,R)-IQNP shows higher brain and heart uptake in rats than IDEX and 4IQNB
- Oak Ridge National Lab., TN (United States); and others
Z-(R)-1-Azabicyclo[2.2.2]oct-3-yl (R)-{alpha}-hydroxy-{alpha}-(1-iodo-1-propen-3-yl)-{alpha}-phenylacetate (Z-(R,R)-IQNP) shows potential for the in vivo imaging of muscarinic receptors (mAChR) by SPECT. In vivo biodistribution studies show high uptake and prolonged retention in areas of the brain containing mAChR. We compared the biodistribution of Z-(R,R)-IQNP with 4-iodoexetimide (IDEX) and R-3 quinuclidinyl S-4-iodobenzilate (41QNB), two established muscarinic imaging agents. IDEX was labeled with iodine-125, 4IQNB was labeled with iodine-131 and IQNP was labeled with iodine-123. A solution containing the three compounds was injected in the same rat (n=5/time point). Animals were sacrificed at 30, 120, and 240 minutes and the levels of the three radioisotopes determined in various tissues. Z-(R,R)-IQNP was retained at twice the level as compared to IDEX and significantly higher than 4-IQNB in the hear and regions of the brain (Table). Z-(R,R)-IQNP also demonstrated low liver uptake as compared to IDEX. These data indicate that Z-(R,R)-IQNP is an attractive candidate for the imaging of mAChR by SPECT.
- DOE Contract Number:
- AC05-96OR22464
- OSTI ID:
- 447779
- Report Number(s):
- CONF-960659--
- Journal Information:
- Journal of Nuclear Medicine, Journal Name: Journal of Nuclear Medicine Journal Issue: Suppl.5 Vol. 37; ISSN JNMEAQ; ISSN 0161-5505
- Country of Publication:
- United States
- Language:
- English
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