Radiation exposure by (-)-F18-NCFHEB, a new PET tracer for imaging of cerebral alpha4beta2 nicotinic acetylcholine receptors (nAChRs)


Radiation exposure by (-)-F18-NCFHEB, a new PET tracer for imaging of cerebral alpha4beta2 nicotinic acetylcholine receptors (nAChRs)

Sattler, B.; Wilke, S.; Starke, A.; Patt, M.; Hoepping, A.; Graef, S.; Schoenknecht, P.; Hegerl, U.; Brust, P.; Sabri, O.

Objectives : (-)-[F-18]Norchloro-fluoro-homoepibatidine ((-)-NCFHEB) is a new tracer for neuroimaging of alpha4beta2 nAChRs with PET. To assess the radiation risk after application of the radioligand, the biodistribution, organ doses (OD) and the effective dose (ED) were determined in a phase 0/1 trial.
Methods : Whole body dosimetry of (-)-NCFHEB was performed in 3 healthy volunteers (59.6±3.9a; weight 74.3±3.1kg; 2m, 1f). The subjects were sequentially imaged up to 7h post i.v. injection of 353.7±10.2 MBq of (-)-NCFHEB on a SIEMENS Biograph16 PET/CT-system with 9 bed positions (BP) per frame, 1.5-6min/BP, CT-attenuation correction and iterative reconstruction. All relevant organs were defined by volumes of interest. Exponential curves were fitted to the time-activity-data. The ODs were calculated using the adult male model with OLINDA. The ED was calculated using tissue weighing factors as published in the ICRP 103/2007.
Results : The highest OD was received by the urinary bladder (80.2±37.8), followed by liver (44.7±5.4) and kidneys (38.6±5.1). The highest contribution to the ED was by the lungs (3.7±0.6) and the urinary bladder (3.2±1.5). The ED by i.v. application of (-)-NCFHEB is 22.9±0.7 (all in [μSv/MBq]).
Conclusions : The ED after i.v. application of 300 MBq (-)-NCFHEB is 6.8±0.2mSv. This corresponds to values obtained with other [F-18]-labeled compounds. These favorable dosimetry data encourage the further development of (-)-NCFHEB as a clinical tool for imaging of alpha4beta2 nAChRs with PET.

  • Poster
    SNM 58th Annual Meeting, 04.-08.06.2011, San Antonio, Texas, USA
  • Abstract in refereed journal
    Journal of Nuclear Medicine 52(2011), 1459

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Publ.-Id: 15450