TABLE I.
Study | Species of subjects |
Sample size | Radiotracer | Duration in minutes of scan after start of radiotracer administration |
Form of radiotracer administration |
Method of plasma sampling for modeling |
Method of modeling |
Conclusion |
---|---|---|---|---|---|---|---|---|
Current (presented in abstract by Brasic et al., 2001; Musachio et al., 2001; Wong et al., 2001, 2002a) | Humans (Homo sapiens) | 6 smokers, 6 nonsmokers including 2 nonsmokers with secondhand smoke exposure | 5-[123I]IA | 300 | 7 B 5 B + CI | Column-switch HPLC (Hilton et al., 2000) | DV estimation by kinetic analysis (Zhou et al., 2001) |
|
Baldwin et al., 2006 | Baboons (Papio anubis) | 1 without nicotine exposure | 5-[123I]IA | 90 | 1 B | HPLC | DV estimation by kinetic analysis |
|
Bottlaender et al., 2003 | Humans (Homo sapiens) | 3 nonsmokers | 2-[18F]FA | 120 | 3 B | Radioactivity measurements corrected for physical decay | Regions of interest on PET scans |
|
Brody et al., 2006 | Humans (Homo sapiens) | 11 smokers with tobacco dependence | 2-[18F]FA | 500 | 11 B + CI before and after cigarette smoking | Gas chromatography with nitrogen-phosphorus detection (Jacob et al., 1981) | Maximal fractional displacement of radioactivity | α4 β2* nAChRs are occupied almost fully in cigarette smokers with tobacco dependence. |
Brust et al., 2008 | Pigs (mixed German landrace and Pietrain) | 24 | (−)-[18F]NCFHEB, (+)- [18F]NCFHEB, 2- [18F]FA | 420 | 24 CI | HPLC | Kinetic analysis with BioMedical Image Quantification Software PMOD Version 2.75 (PMOD Technologies, Zurich, Switzerland) |
|
Chefer et al., 1998 | Rhesus monkeys (Macaca mulatta) | 1 | 5-[123I]IA | 270 | B | HPLC | Kinetic analysis with cerebellum as the reference tissue | 5-[123 I]IA is safe and efficacious for brain imaging in monkeys. |
Chefer et al., 1999 | Rhesus monkeys (Macaca mulatta) | 2 | 2-[18F]FA | 240 | 2 B+CI | HPLC | Kinetic analysis with cerebellum as the reference tissue |
|
Chefer et al., 2008 | Rhesus monkeys (Macaca mulatta) | 3 | [18F]NIDA522131 and 2-[18F]FA | 540 | 3 B | HPLC | Kinetic analysis with BioMedical Image Quantification Software PMOD Version 2.75 (PMOD Technologies, Zurich, Switzerland) |
|
Colloby et al., 2008 | Humans (Homo sapiens) | 9 (4 AD, 5 DLB) | 5-[123I]IA before and after administration of donepezil | 120 | B | none | SPM2 |
|
Cosgrove et al., 2007 | Humans (Homo sapiens) | 29 nonsmokers (10 men, 19 women) | 5-[123I]IA during early follicular and mid-luteal phases in women | 480 | B + CI | HPLC | MEDx software (Medical Numerics, Inc.) |
|
Ding et al., 2000 | Baboons (Papio anubis) | 1 | 2-[18F]FA and 6-[18F]FA | 180 | B | HPLC | Kinetic analysis |
|
Dollé et al., 1999 | Baboons (Papio papio) and Rhesus monkey (Macaca mulatta) | 1 baboon and 1 monkey | 2-[18F]FA; 5-[123I]IA; [18F]fluoronorchloroepibatidine | 90 | B | HPLC | Kinetic analysis |
|
Fujita et al., 2006 | Humans (Homo sapiens) | 15 healthy; 10 PD | 5-[123I]IA | 230 | B | HPLC | Kinetic analysis |
|
Fujita et al., 2002 | Humans (Homo sapiens) | 10 | 5-[123I]IA | 1440 | B | HPLC | Kinetic analysis |
|
Fujita et al., 2000 | Baboons | 3 | 5-[123I]IA | 289–495 | B, B + CI | HPLC | Kinetic analysis | 5-[123I]IA is safe, efficacious in baboons. |
Gallezot et al., 2005 | Humans (Homo sapiens) | 7 nonsmokers | 2-[18F]FA | 210 | B | HPLC | Kinetic analysis |
|
Horti et al., 2000 | Rhesus monkeys (Macaca mulatta) | 2 | 6-[18F]FA | 270 | B | HPLC | Kinetic analysis |
|
Ishizu et al., 2004 | Humans (Homo sapiens) | 4 | 5-[123I]IA | 360 | B | Arterial blood sampling | Kinetic analysis |
|
Kassiou et al., 2001 | Baboons (Papio hamadryas) | 2 | 5-[123I]IA | 180 | B | Plasma metabolite analysis | Kinetic analysis |
|
Kassiou et al., 2002 | Baboons (Papio papio) | 3 | [76Br]BrPH | 132 to 240 | B | Plasma metabolite analysis | Kinetic analysis | [76Br]BrPH is safe and efficacious in baboons. |
Kimes et al., 2003 | Humans (Homo sapiens) and Rhesus monkeys (Macaca mulatta) | 6 humans and 2 monkeys | 2-[18F]FA | 420 to 480 | B | Plasma metabolite analysis | Kinetic analysis |
|
Mamede et al., 2004 | Humans (Homo sapiens) | 21 humans | 5-[123I]IA | 90 or 360 | B | TLC | Kinetic analysis |
|
Mamede et al., 2007 | Humans (Homo sapiens) | 16 (6 nonsmokers and 10 smoders) | 5-[123I]IA | 360 | B | TLC | Kinetic analysis |
|
Mitkovski et al., 2005 | Humans (Homo sapiens) | 10 | 2-[18F]FA | 120 | B | Arterial blood sampling | Kinetic analysis |
|
Mitsis et al., 2007 | Humans (Homo sapiens) | unknown | 5-[123I]IA | 480 | B + CI | Venous sampling | Kinetic analysis |
|
O’Brien et al., 2007 | Humans (Homo sapiens) | 32 (16 healthy and 16 AD) | 5-[123I]IA | 150 | B | HPLC | Kinetic analysis |
|
Obrzut et al., 2005 | Humans (Homo sapiens) | 2 | 2-[18F]FA | 180 | B | plasma sampling | Kinetic analysis |
|
Oishi et al., 2006, 2007 | Humans (Homo sapiens) | 10 healthy and 10 PD | 5-[123I]IA | 240 | B | Arterial blood sampling | Kinetic analysis |
|
Picard et al., 2006 | Humans (Homo sapiens) | 7 healthy and 8 ADNFLE | 2-[18F]FA | 240 | B | Venous plasma sampling | SPM2 |
|
Saji et al., 2002 | Common marmoset (Callithrix jacchus)I | 1 | 5-[123I]IA | 240 | B | Venous plasma sampling | Kinetic analysis |
|
Sorger et al., 2007 | Humans (Homo sapiens) | 12 healthy and 97 patients with neurological disorders | 2-[18F]FA | 420 | B | HPLC or TLC | Kinetic analysis |
|
Staley et al., 2005 | Humans (Homo sapiens) | 10 | 5-[123I]IA | 420 | B + CI | Plasma sampling | SPM99 |
|
Staley et al., 2006 | Humans (Homo sapiens) and Rhesus monkeys (Macaca mulatta) | 32 humans (16 nonsmokers and 16 smokers) and two monkeys | 5-[123I]IA | 480 | B + CI | Plasma sampling | Kinetic analysis |
|
Ueda et al., 2004 | Humans (Homo sapiens) | 4 | 5-[123I]IA | 1440 | B | Plasma sampling | Kinetic analysis |
|
Valette et al., 1999 | Baboons (Papio papio) | 3 | 2-[18F]FA | 180 | B | Plasma sampling | Kinetic analysis |
|
Wüllner et al., 2007 | Humans (Homo sapiens) | 14 (7 nonsmokers and 7 smokers) | 2-[18F]FA | 364 | CI | HPLC | SPM2 |
|
Yoshida et al., 2002 | Humans (Homo sapiens) | 6 healthy and 5 AD | 5-[123I]IA | 60 | CI | Arterial blood sampling | Kinetic analysis |
|
[76Br]BrPH = [76Br]norchlorobromoepibatidine; [18F]NCFHEB = [18F]norchloro-fluoro-homoepibatidine; [18F]NIDA522131 = chloro-3-((2-(S)-azetidinyl)methoxy)-5-(2-[18F]fluoropyridin-4-yl)pyridine; 2-[18F]FA = 2-[18F]fluoro-3-(2(S)-azetidinylmethoxy)pyridine; 5-[123I]IA = (S)-5-[123I]iodo-3-(2-azetidinylmethoxy)pyridine; 6-[18F]FA = 6-[18F]fluoro-3-(2(S)-azetidinylmethoxy)pyridine; AD = Alzheimer’s disease; ADNFLE = autosomal dominant nocturnal frontal lobe epilepsy; B = bolus; B + CI = bolus and continuous infusion; CI = continuous infusion; DLB = dementia with Lewy bodies; DV = distribution volume; HPLC = high performance lipid chromatography; nAChRs = nicotinic acetylcholine receptors; PD = Parkinson’s disease; PET = positron emission tomography; SPECT = single photon emission computed tomography; SPM2 = Statistical Parametric Mapping 2 (http://www.fil.ion.ucl.ac.uk/spm/); SPM99 = Statistical Parametric Mapping, version 99; TLC = thin layer chromatography.