Approaches to quantify radioligands that wash out slowly from target organs
As a general approach to radioligands with slow kinetics, studies in animals should be used to determine key pharmacological properties, like reversibility, of the radio-ligand; that long scans (and sometimes atypically long scans) be used to identify slow rate constants; and that retest studies can...
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| Published in | European journal of nuclear medicine and molecular imaging Vol. 37; no. 5; pp. 917 - 919 |
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| Main Authors | , , , , |
| Format | Journal Article |
| Language | English |
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Berlin/Heidelberg
Springer-Verlag
01.05.2010
Springer Nature B.V |
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| Abstract | As a general approach to radioligands with slow kinetics, studies in animals should be used to determine key pharmacological properties, like reversibility, of the radio-ligand; that long scans (and sometimes atypically long scans) be used to identify slow rate constants; and that retest studies can be unusually useful to identify sources of error in measurements of brain uptake and the concentration of radioligand in plasma, as well as in distribution volume, which is a ratio of brain to plasma measurements. |
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| AbstractList | As a general approach to radioligands with slow kinetics, studies in animals should be used to determine key pharmacological properties, like reversibility, of the radio-ligand; that long scans (and sometimes atypically long scans) be used to identify slow rate constants; and that retest studies can be unusually useful to identify sources of error in measurements of brain uptake and the concentration of radioligand in plasma, as well as in distribution volume, which is a ratio of brain to plasma measurements. |
| Author | Halldin, Christer Innis, Robert B. Hirvonen, Jussi Terry, Garth E. Pike, Victor W. |
| Author_xml | – sequence: 1 givenname: Jussi surname: Hirvonen fullname: Hirvonen, Jussi organization: Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health – sequence: 2 givenname: Garth E. surname: Terry fullname: Terry, Garth E. organization: Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health – sequence: 3 givenname: Christer surname: Halldin fullname: Halldin, Christer organization: Department of Clinical Neuroscience, Psychiatry Section, Karolinska Institutet – sequence: 4 givenname: Victor W. surname: Pike fullname: Pike, Victor W. organization: Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health – sequence: 5 givenname: Robert B. surname: Innis fullname: Innis, Robert B. email: robert.innis@nih.gov organization: Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health |
| BackLink | https://www.ncbi.nlm.nih.gov/pubmed/20358196$$D View this record in MEDLINE/PubMed http://kipublications.ki.se/Default.aspx?queryparsed=id:120301534$$DView record from Swedish Publication Index |
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| CitedBy_id | crossref_primary_10_1016_j_biopsych_2015_08_021 crossref_primary_10_1016_j_bpsc_2015_09_008 crossref_primary_10_1038_jcbfm_2015_46 crossref_primary_10_1021_acschemneuro_5b00066 crossref_primary_10_1016_j_neuroimage_2014_05_050 crossref_primary_10_1021_acs_jmedchem_0c01459 crossref_primary_10_1002_mp_12732 crossref_primary_10_1016_j_euroneuro_2018_12_014 crossref_primary_10_1007_s00259_010_1518_x crossref_primary_10_2310_7290_2014_00004 crossref_primary_10_1002_prp2_253 crossref_primary_10_1007_s00259_011_1954_2 crossref_primary_10_1111_adb_13061 crossref_primary_10_1002_mds_29117 crossref_primary_10_1111_bph_12505 |
| Cites_doi | 10.1038/jcbfm.1994.56 10.1073/pnas.0703472104 10.1007/s00259-009-1340-5 10.1002/ana.410150302 10.1016/0006-8993(84)91113-2 10.2967/jnumed.109.067074 10.1038/sj.npp.1301402 10.1002/syn.20728 10.1038/sj.jcbfm.9600493 10.1016/j.neuroimage.2009.06.059 |
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| References | BurnsHDVan LaereKSanabria-BohórquezSHamillTGBormansGEngWS[18F]MK-9470, a positron emission tomography (PET) tracer for in vivo human PET brain imaging of the cannabinoid-1 receptorProc Natl Acad Sci U S A2007104239800980510.1073/pnas.07034721041:CAS:528:DC%2BD2sXmsFSmsLc%3D17535893 LaruelleMAbi-DarghamAal-TikritiMSBaldwinRMZea-PonceYZoghbiSSSPECT quantification of [123I]iomazenil binding to benzodiazepine receptors in nonhuman primates: II. Equilibrium analysis of constant infusion experiments and correlation with in vitro parametersJ Cereb Blood Flow Metab19941434534651:CAS:528:DyaK2cXkslOnsbc%3D8163587 TerryGEHirvonenJLiowJSZoghbiSSGladdingRTauscherJTImaging and quantitation of cannabinoid CB1 receptors in human and monkey brains using (18)F-labeled inverse agonist radioligandsJ Nucl Med201051111212010.2967/jnumed.109.0670741:CAS:528:DC%2BC3cXhsFCrsbs%3D20008988 TerryGELiowJSZoghbiSSHirvonenJFarrisAGLernerAQuantitation of cannabinoid CB1 receptors in healthy human brain using positron emission tomography and an inverse agonist radioligandNeuroimage200948236237010.1016/j.neuroimage.2009.06.05919573609 ItohTAbeKHongJInoueOPikeVWInnisRBEffects of cAMP-dependent protein kinase activator and inhibitor on in vivo rolipram binding to phosphodiesterase 4 in conscious ratsSynapse201064217217610.1002/syn.207281:CAS:528:DC%2BD1MXhsFWrsb3K19852069 FrostJJWagnerHNJrKinetics of binding to opiate receptors in vivo predicted from in vitro parametersBrain Res1984305111110.1016/0006-8993(84)91113-21:CAS:528:DyaL2cXksVyls78%3D6331593 InnisRBCunninghamVJDelforgeJFujitaMGjeddeAGunnRNConsensus nomenclature for in vivo imaging of reversibly binding radioligandsJ Cereb Blood Flow Metab20072791533153910.1038/sj.jcbfm.96004931:CAS:528:DC%2BD2sXptlSqtrc%3D17519979 MintunMARaichleMEKilbournMRWootenGFWelchMJA quantitative model for the in vivo assessment of drug binding sites with positron emission tomographyAnn Neurol19841521722710.1002/ana.4101503021:CAS:528:DyaL2cXitVejur0%3D6609679 Sanabria-Bohórquez SM, Hamill TG, Goffin K, De Lepeleire I, Bormans G, Burns HD, et al. Kinetic analysis of the cannabinoid-1 receptor PET tracer [(18)F]MK-9470 in human brain. Eur J Nucl Med Mol Imaging 2009. doi:10.1007/s00259-009-1340-5. YasunoFBrownAKZoghbiSSKrushinskiJHChernetETauscherJThe PET radioligand [11C]MePPEP binds reversibly and with high specific signal to cannabinoid CB1 receptors in nonhuman primate brainNeuropsychopharmacology20083325926910.1038/sj.npp.13014021:CAS:528:DC%2BD2sXhsVSktrrI17392732 GE Terry (1426_CR4) 2009; 48 T Itoh (1426_CR5) 2010; 64 MA Mintun (1426_CR6) 1984; 15 HD Burns (1426_CR2) 2007; 104 F Yasuno (1426_CR9) 2008; 33 M Laruelle (1426_CR7) 1994; 14 RB Innis (1426_CR8) 2007; 27 JJ Frost (1426_CR10) 1984; 305 GE Terry (1426_CR3) 2010; 51 1426_CR1 20033684 - Eur J Nucl Med Mol Imaging. 2010 May;37(5):920-33. doi: 10.1007/s00259-009-1340-5. 20577739 - Eur J Nucl Med Mol Imaging. 2010 Aug;37(8):1613-5. doi: 10.1007/s00259-010-1518-x. |
| References_xml | – reference: TerryGEHirvonenJLiowJSZoghbiSSGladdingRTauscherJTImaging and quantitation of cannabinoid CB1 receptors in human and monkey brains using (18)F-labeled inverse agonist radioligandsJ Nucl Med201051111212010.2967/jnumed.109.0670741:CAS:528:DC%2BC3cXhsFCrsbs%3D20008988 – reference: TerryGELiowJSZoghbiSSHirvonenJFarrisAGLernerAQuantitation of cannabinoid CB1 receptors in healthy human brain using positron emission tomography and an inverse agonist radioligandNeuroimage200948236237010.1016/j.neuroimage.2009.06.05919573609 – reference: MintunMARaichleMEKilbournMRWootenGFWelchMJA quantitative model for the in vivo assessment of drug binding sites with positron emission tomographyAnn Neurol19841521722710.1002/ana.4101503021:CAS:528:DyaL2cXitVejur0%3D6609679 – reference: BurnsHDVan LaereKSanabria-BohórquezSHamillTGBormansGEngWS[18F]MK-9470, a positron emission tomography (PET) tracer for in vivo human PET brain imaging of the cannabinoid-1 receptorProc Natl Acad Sci U S A2007104239800980510.1073/pnas.07034721041:CAS:528:DC%2BD2sXmsFSmsLc%3D17535893 – reference: Sanabria-Bohórquez SM, Hamill TG, Goffin K, De Lepeleire I, Bormans G, Burns HD, et al. Kinetic analysis of the cannabinoid-1 receptor PET tracer [(18)F]MK-9470 in human brain. Eur J Nucl Med Mol Imaging 2009. doi:10.1007/s00259-009-1340-5. – reference: FrostJJWagnerHNJrKinetics of binding to opiate receptors in vivo predicted from in vitro parametersBrain Res1984305111110.1016/0006-8993(84)91113-21:CAS:528:DyaL2cXksVyls78%3D6331593 – reference: LaruelleMAbi-DarghamAal-TikritiMSBaldwinRMZea-PonceYZoghbiSSSPECT quantification of [123I]iomazenil binding to benzodiazepine receptors in nonhuman primates: II. Equilibrium analysis of constant infusion experiments and correlation with in vitro parametersJ Cereb Blood Flow Metab19941434534651:CAS:528:DyaK2cXkslOnsbc%3D8163587 – reference: InnisRBCunninghamVJDelforgeJFujitaMGjeddeAGunnRNConsensus nomenclature for in vivo imaging of reversibly binding radioligandsJ Cereb Blood Flow Metab20072791533153910.1038/sj.jcbfm.96004931:CAS:528:DC%2BD2sXptlSqtrc%3D17519979 – reference: YasunoFBrownAKZoghbiSSKrushinskiJHChernetETauscherJThe PET radioligand [11C]MePPEP binds reversibly and with high specific signal to cannabinoid CB1 receptors in nonhuman primate brainNeuropsychopharmacology20083325926910.1038/sj.npp.13014021:CAS:528:DC%2BD2sXhsVSktrrI17392732 – reference: ItohTAbeKHongJInoueOPikeVWInnisRBEffects of cAMP-dependent protein kinase activator and inhibitor on in vivo rolipram binding to phosphodiesterase 4 in conscious ratsSynapse201064217217610.1002/syn.207281:CAS:528:DC%2BD1MXhsFWrsb3K19852069 – volume: 14 start-page: 453 issue: 3 year: 1994 ident: 1426_CR7 publication-title: J Cereb Blood Flow Metab doi: 10.1038/jcbfm.1994.56 – volume: 104 start-page: 9800 issue: 23 year: 2007 ident: 1426_CR2 publication-title: Proc Natl Acad Sci U S A doi: 10.1073/pnas.0703472104 – ident: 1426_CR1 doi: 10.1007/s00259-009-1340-5 – volume: 15 start-page: 217 year: 1984 ident: 1426_CR6 publication-title: Ann Neurol doi: 10.1002/ana.410150302 – volume: 305 start-page: 1 issue: 1 year: 1984 ident: 1426_CR10 publication-title: Brain Res doi: 10.1016/0006-8993(84)91113-2 – volume: 51 start-page: 112 issue: 1 year: 2010 ident: 1426_CR3 publication-title: J Nucl Med doi: 10.2967/jnumed.109.067074 – volume: 33 start-page: 259 year: 2008 ident: 1426_CR9 publication-title: Neuropsychopharmacology doi: 10.1038/sj.npp.1301402 – volume: 64 start-page: 172 issue: 2 year: 2010 ident: 1426_CR5 publication-title: Synapse doi: 10.1002/syn.20728 – volume: 27 start-page: 1533 issue: 9 year: 2007 ident: 1426_CR8 publication-title: J Cereb Blood Flow Metab doi: 10.1038/sj.jcbfm.9600493 – volume: 48 start-page: 362 issue: 2 year: 2009 ident: 1426_CR4 publication-title: Neuroimage doi: 10.1016/j.neuroimage.2009.06.059 – reference: 20033684 - Eur J Nucl Med Mol Imaging. 2010 May;37(5):920-33. doi: 10.1007/s00259-009-1340-5. – reference: 20577739 - Eur J Nucl Med Mol Imaging. 2010 Aug;37(8):1613-5. doi: 10.1007/s00259-010-1518-x. |
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| Title | Approaches to quantify radioligands that wash out slowly from target organs |
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