메뉴 건너뛰기




Volumn 23, Issue 18, 2016, Pages 1818-1869

Considerations in the development of reversibly binding pet radioligands for brain imaging

Author keywords

Blood brain barrier; Carbon 11; Efflux transporter; Fluorine 18; Molecular imaging; PET; Positron emitter; Radioligand

Indexed keywords

BRAIN PROTEIN; CARBON 11; FLUORINE 18; RADIOLIGAND; LIGAND; PROTEIN; RADIOISOTOPE;

EID: 84978077114     PISSN: 09298673     EISSN: 1875533X     Source Type: Journal    
DOI: 10.2174/0929867323666160418114826     Document Type: Review
Times cited : (152)

References (387)
  • 1
    • 33749234216 scopus 로고    scopus 로고
    • Drugs, their targets and the nature and number of drug targets
    • Imming, P.; Sinning, C.; Meyer, A. Drugs, their targets and the nature and number of drug targets. Nature Rev., 2007, 5, 821-834.
    • (2007) Nature Rev. , vol.5 , pp. 821-834
    • Imming, P.1    Sinning, C.2    Meyer, A.3
  • 2
    • 33744494881 scopus 로고    scopus 로고
    • Brain receptor imaging
    • Heiss, W.D.; Herholz, K. Brain receptor imaging. J. Nucl. Med., 2006, 47, 302-312.
    • (2006) J. Nucl. Med. , vol.47 , pp. 302-312
    • Heiss, W.D.1    Herholz, K.2
  • 3
    • 84867337416 scopus 로고    scopus 로고
    • Positron emission tomography imaging in neurological disorders
    • Politis, M.; Piccini, P. Positron emission tomography imaging in neurological disorders. J. Neurol., 2012, 259, 1769-1780.
    • (2012) J. Neurol. , vol.259 , pp. 1769-1780
    • Politis, M.1    Piccini, P.2
  • 4
    • 84873522293 scopus 로고    scopus 로고
    • Neuroreceptor imaging in depression
    • Savitz, J.B.; Drevets, W.C. Neuroreceptor imaging in depression. Neurobiol. Dis., 2013, 52, 49-65.
    • (2013) Neurobiol. Dis. , vol.52 , pp. 49-65
    • Savitz, J.B.1    Drevets, W.C.2
  • 5
    • 38349095953 scopus 로고    scopus 로고
    • The role of molecular imaging in drug discovery and development
    • Hargreaves, R.J. The role of molecular imaging in drug discovery and development. Clin. Pharmacol. Ther., 2008, 83, 349-353.
    • (2008) Clin. Pharmacol. Ther. , vol.83 , pp. 349-353
    • Hargreaves, R.J.1
  • 6
    • 0029937457 scopus 로고    scopus 로고
    • The advantage of using positron emission tomography in drug research
    • Farde, L. The advantage of using positron emission tomography in drug research. Trends Neurosci., 1996, 19, 211-214.
    • (1996) Trends Neurosci. , vol.19 , pp. 211-214
    • Farde, L.1
  • 8
    • 84913593388 scopus 로고    scopus 로고
    • Positron emission tomography in CNS drug discovery and drug monitoring
    • Piel, M.; Vernaleken, I.; Rösch, F. Positron emission tomography in CNS drug discovery and drug monitoring. J. Med. Chem., 2014, 57, 9232-9258.
    • (2014) J. Med. Chem. , vol.57 , pp. 9232-9258
    • Piel, M.1    Vernaleken, I.2    Rösch, F.3
  • 10
    • 53549101899 scopus 로고    scopus 로고
    • Synthesis and biological evaluation of one novel technetium-99m-labeled nitroquipazine derivative as an imaging agent for serotonin transporter
    • Guo, Y.; Chen, X.; Jia, H.; Ji, X.; Liu, B. Synthesis and biological evaluation of one novel technetium-99m-labeled nitroquipazine derivative as an imaging agent for serotonin transporter. Appl. Radiat. Isot., 2008, 66, 1804-1809.
    • (2008) Appl. Radiat. Isot. , vol.66 , pp. 1804-1809
    • Guo, Y.1    Chen, X.2    Jia, H.3    Ji, X.4    Liu, B.5
  • 11
    • 0027241271 scopus 로고
    • Positron-emitting radioligands for studies in vivo - Probes for human psychopharmacology
    • Pike, V.W. Positron-emitting radioligands for studies in vivo - probes for human psychopharmacology. J. Psychopharmacology, 1993, 7, 139-158.
    • (1993) J. Psychopharmacology , vol.7 , pp. 139-158
    • Pike, V.W.1
  • 12
    • 0030830518 scopus 로고    scopus 로고
    • In vivo imaging of neurotransmitter systems using radiolabeled receptor ligands
    • Kegeles, L.S.; Mann, J.J. In vivo imaging of neurotransmitter systems using radiolabeled receptor ligands. Neuropsychopharmacology, 1997, 17, 293-307.
    • (1997) Neuropsychopharmacology , vol.17 , pp. 293-307
    • Kegeles, L.S.1    Mann, J.J.2
  • 13
    • 0034931817 scopus 로고    scopus 로고
    • Brain radioligands - State of the art and new trends
    • Halldin, C.; Gulyás, B.; Langer, O.; Farde, L. Brain radioligands - state of the art and new trends. Q. J. Nucl. Med., 2001, 45, 139-152.
    • (2001) Q. J. Nucl. Med. , vol.45 , pp. 139-152
    • Halldin, C.1    Gulyás, B.2    Langer, O.3    Farde, L.4
  • 14
    • 0344983883 scopus 로고    scopus 로고
    • Relationships between radiotracer properties and image quality in molecular imaging of the brain with positron emission tomography
    • Laruelle, M.; Slifstein, M.; Huang, Y. Relationships between radiotracer properties and image quality in molecular imaging of the brain with positron emission tomography. Mol. Imaging Biol., 2003, 5, 363-375.
    • (2003) Mol. Imaging Biol. , vol.5 , pp. 363-375
    • Laruelle, M.1    Slifstein, M.2    Huang, Y.3
  • 15
    • 0344121285 scopus 로고    scopus 로고
    • Predicting the success of a radiopharmaceutical for in vivo imaging of central nervous system neuroreceptor systems
    • Wong, D.F.; Pomper, M.G. Predicting the success of a radiopharmaceutical for in vivo imaging of central nervous system neuroreceptor systems. Mol. Imaging Biol., 2003, 5, 350-362.
    • (2003) Mol. Imaging Biol. , vol.5 , pp. 350-362
    • Wong, D.F.1    Pomper, M.G.2
  • 16
    • 33646550152 scopus 로고    scopus 로고
    • Discussion of targeting proteins in vivo: In vitro guidelines
    • Eckelman, W.C.; Kilbourn, M.R.; Mathis, C.A. Discussion of targeting proteins in vivo: in vitro guidelines. Nucl. Med. Biol., 2006, 33, 449-451.
    • (2006) Nucl. Med. Biol. , vol.33 , pp. 449-451
    • Eckelman, W.C.1    Kilbourn, M.R.2    Mathis, C.A.3
  • 17
    • 56549113643 scopus 로고    scopus 로고
    • In vivo site-directed radiotracers: A mini-review
    • Patel, S.; Gibson, R. In vivo site-directed radiotracers: a mini-review. Nucl. Med. Biol., 2008, 35, 805-815.
    • (2008) Nucl. Med. Biol. , vol.35 , pp. 805-815
    • Patel, S.1    Gibson, R.2
  • 19
    • 84919832051 scopus 로고    scopus 로고
    • 18F-labeled radiotracers for neuroreceptor imaging with positron emission tomography
    • 18F-labeled radiotracers for neuroreceptor imaging with positron emission tomography. Neurosci. Bull., 2014, 30, 777-811.
    • (2014) Neurosci. Bull. , vol.30 , pp. 777-811
    • Brust, P.1    Van-Den-Hoff, J.2    Steinbach, J.3
  • 20
    • 84878763239 scopus 로고    scopus 로고
    • Modeling of PET data in CNS drug discovery and development
    • Varnäs, K.; Varrone, A.; Farde, L. Modeling of PET data in CNS drug discovery and development. J. Pharmokinet. Pharmacodyn., 2013, 40, 267-279.
    • (2013) J. Pharmokinet. Pharmacodyn. , vol.40 , pp. 267-279
    • Varnäs, K.1    Varrone, A.2    Farde, L.3
  • 21
    • 84936125907 scopus 로고    scopus 로고
    • Quantitative imaging of protein targets in the human brain with PET
    • Gunn, R.N.; Slifstein, M.; Searle, G.E.; Price, J.C. Quantitative imaging of protein targets in the human brain with PET. Phys. Med. Biol., 2015, 60, R363-R411.
    • (2015) Phys. Med. Biol. , vol.60 , pp. R363-R411
    • Gunn, R.N.1    Slifstein, M.2    Searle, G.E.3    Price, J.C.4
  • 22
    • 0021364348 scopus 로고
    • A quantitative model for the in vivo assessment of drug binding sites with positron emission tomography
    • Mintun, M.A.; Raichle, M.E.; Kilbourn, M.R.; Wooten, G.F.; Welch, M.J. A quantitative model for the in vivo assessment of drug binding sites with positron emission tomography. Ann. Neurol., 1984, 15, 217-227.
    • (1984) Ann. Neurol. , vol.15 , pp. 217-227
    • Mintun, M.A.1    Raichle, M.E.2    Kilbourn, M.R.3    Wooten, G.F.4    Welch, M.J.5
  • 25
    • 0030468875 scopus 로고    scopus 로고
    • Simplified reference tissue model for PET receptor studies
    • Lammertsma, A.A.; Hume, S.P. Simplified reference tissue model for PET receptor studies. NeuroImage, 1996, 4, 153-158.
    • (1996) NeuroImage , vol.4 , pp. 153-158
    • Lammertsma, A.A.1    Hume, S.P.2
  • 26
    • 0031279782 scopus 로고    scopus 로고
    • Parametric imaging of ligand-receptor binding in PET using a simplified reference region model
    • Gunn, R.N.; Lammertsma, A.A.; Hume, S.P.; Cunningham, V.J. Parametric imaging of ligand-receptor binding in PET using a simplified reference region model. NeuroImage, 1997, 6, 279-287.
    • (1997) NeuroImage , vol.6 , pp. 279-287
    • Gunn, R.N.1    Lammertsma, A.A.2    Hume, S.P.3    Cunningham, V.J.4
  • 29
    • 0033729522 scopus 로고    scopus 로고
    • Graphical analysis of PET data applied to reversible and irreversible tracers
    • Logan, J. Graphical analysis of PET data applied to reversible and irreversible tracers. Nucl. Med. Biol., 2000, 27, 661-670.
    • (2000) Nucl. Med. Biol. , vol.27 , pp. 661-670
    • Logan, J.1
  • 32
    • 0022595579 scopus 로고
    • 2 receptor binding in the living human brain by PET
    • 2 receptor binding in the living human brain by PET. Science, 1986, 231, 258-261.
    • (1986) Science , vol.231 , pp. 258-261
    • Farde, L.1    Hall, H.2    Ehrin, E.3    Sedvall, G.4
  • 35
    • 0030939401 scopus 로고    scopus 로고
    • Parametric images of benzodiazepine receptor concentration using a partial-saturation injection
    • Delforge, J.; Spelle, L.; Bendriem, B.; Samson, Y.; Syrota, A. Parametric images of benzodiazepine receptor concentration using a partial-saturation injection. J. Cereb. Blood Flow Metab., 1997, 17, 343-355.
    • (1997) J. Cereb. Blood Flow Metab. , vol.17 , pp. 343-355
    • Delforge, J.1    Spelle, L.2    Bendriem, B.3    Samson, Y.4    Syrota, A.5
  • 36
    • 84855184017 scopus 로고    scopus 로고
    • Serotonin-1A receptors in major depression quantified using PET: Controversies, confounds, and recommendations
    • Shrestha, S.; Hirvonen, J.; Hines, C.S.; Henter, I.; Svenningsson, P.; Pike, V.W.; Innis, R.B. Serotonin-1A receptors in major depression quantified using PET: controversies, confounds, and recommendations. NeuroImage, 2012, 59, 3243-3251.
    • (2012) NeuroImage , vol.59 , pp. 3243-3251
    • Shrestha, S.1    Hirvonen, J.2    Hines, C.S.3    Henter, I.4    Svenningsson, P.5    Pike, V.W.6    Innis, R.B.7
  • 37
    • 84869021291 scopus 로고    scopus 로고
    • Development of positron emission tomography β-amyloid plaque imaging agents
    • Mathis, C.A.; Mason, N.S.; Lopresti, B.J.; Klunk, W.E. Development of positron emission tomography β-amyloid plaque imaging agents. Semin. Nucl. Med., 2012, 42, 423-432.
    • (2012) Semin. Nucl. Med. , vol.42 , pp. 423-432
    • Mathis, C.A.1    Mason, N.S.2    Lopresti, B.J.3    Klunk, W.E.4
  • 38
    • 84859761754 scopus 로고    scopus 로고
    • The β-amyloid hypothesis in Alzheimer's disease: Seeing is believing
    • Kung, H.F. The β-amyloid hypothesis in Alzheimer's disease: seeing is believing. ACS Med. Chem. Lett., 2012, 3, 265-267.
    • (2012) ACS Med. Chem. Lett. , vol.3 , pp. 265-267
    • Kung, H.F.1
  • 39
    • 80055083184 scopus 로고    scopus 로고
    • Imaging brain microglial activation using positron emission tomography and translocator protein-specific radioligands
    • Owen, D.R.J.; Matthews, P.M. Imaging brain microglial activation using positron emission tomography and translocator protein-specific radioligands. Int. Rev. Neurobiol., 2011, 101, 19-39.
    • (2011) Int. Rev. Neurobiol. , vol.101 , pp. 19-39
    • Owen, D.R.J.1    Matthews, P.M.2
  • 40
    • 70350455478 scopus 로고    scopus 로고
    • Stroke incidentally identified using improved positron emission tomography for microglial activation
    • Kreisl, W.C.; Mbeo, G.; Fujita, M.; Zoghbi, S.S.; Pike, V.W.; Innis, R.B.; McArthur, J.C. Stroke incidentally identified using improved positron emission tomography for microglial activation. Arch. Neurol., 2009, 66, 1288-1289.
    • (2009) Arch. Neurol. , vol.66 , pp. 1288-1289
    • Kreisl, W.C.1    Mbeo, G.2    Fujita, M.3    Zoghbi, S.S.4    Pike, V.W.5    Innis, R.B.6    McArthur, J.C.7
  • 42
    • 84879901761 scopus 로고    scopus 로고
    • PET radioligand binding to translocator protein correlates with severity of Alzheimer's disease and may mark conversion from mild cognitive impairment
    • Kreisl, W.C.; Lyoo, C.H.; McGwier, M.; Snow, J.; Jenko, K.J.; Corona, W.; Morse, C.L.; Zoghbi, S.S.; Pike, V.W.; McMahon, F.J.; Turner R.S.; Innis, R.B.; Biomarkers Consortium PET Radioligand Project Team. PET radioligand binding to translocator protein correlates with severity of Alzheimer's disease and may mark conversion from mild cognitive impairment. Brain, 2013, 136, 2228-2238.
    • (2013) Brain , vol.136 , pp. 2228-2238
    • Kreisl, W.C.1    Lyoo, C.H.2    McGwier, M.3    Snow, J.4    Jenko, K.J.5    Corona, W.6    Morse, C.L.7    Zoghbi, S.S.8    Pike, V.W.9    McMahon, F.J.10    Turner, R.S.11    Innis, R.B.12
  • 45
    • 84871920442 scopus 로고    scopus 로고
    • A genetic polymorphism for translocator protein 18 kDa affects both in vitro and in vivo radioligand binding in human brain to this putative biomarker of neuroinflammation
    • Kreisl, W.C.; Jenko, K.J.; Hines, C.S.; Lyoo, C.H.; Corona, W.; Morse C.L.; Zoghbi, S.S.; Hyde, T.; Kleinman, J.E.; Pike, V.W.; McMahon, F.J.; Innis, R.B.; Biomarkers Consortium PET Radioligand Project Team. A genetic polymorphism for translocator protein 18 kDa affects both in vitro and in vivo radioligand binding in human brain to this putative biomarker of neuroinflammation. J. Cereb. Blood Flow Metab., 2013, 33, 53-58.
    • (2013) J. Cereb. Blood Flow Metab. , vol.33 , pp. 53-58
    • Kreisl, W.C.1    Jenko, K.J.2    Hines, C.S.3    Lyoo, C.H.4    Corona, W.5    Morse, C.L.6    Zoghbi, S.S.7    Hyde, T.8    Kleinman, J.E.9    Pike, V.W.10    McMahon, F.J.11    Innis, R.B.12
  • 50
    • 77956203458 scopus 로고    scopus 로고
    • Imaging the effects of genetic polymorphisms on radioligand binding in the living human brain: A review on genetic neuroreceptor imaging of monoaminergic systems in psychiatry
    • Willeit, M.; Praschak-Rieder, N. Imaging the effects of genetic polymorphisms on radioligand binding in the living human brain: a review on genetic neuroreceptor imaging of monoaminergic systems in psychiatry. NeuroImage, 2010, 53, 878-892.
    • (2010) NeuroImage , vol.53 , pp. 878-892
    • Willeit, M.1    Praschak-Rieder, N.2
  • 51
    • 0032212773 scopus 로고    scopus 로고
    • Whole hemisphere autoradiography of the postmortem human brain
    • Hall, H.; Halldin, C.; Farde, L.; Sedvall, G. Whole hemisphere autoradiography of the postmortem human brain. Nucl. Med. Biol., 1998, 25, 715-719.
    • (1998) Nucl. Med. Biol. , vol.25 , pp. 715-719
    • Hall, H.1    Halldin, C.2    Farde, L.3    Sedvall, G.4
  • 52
    • 3042776615 scopus 로고    scopus 로고
    • Autoradiographic distribution of serotonin transporters and receptor subtypes in human brain
    • Varnäs, K.; Halldin, C.; Hall, H. Autoradiographic distribution of serotonin transporters and receptor subtypes in human brain. Human Brain Mapping, 2004, 22, 246-260.
    • (2004) Human Brain Mapping , vol.22 , pp. 246-260
    • Varnäs, K.1    Halldin, C.2    Hall, H.3
  • 56
    • 84978091212 scopus 로고
    • Positron emission tomography and autoradiography: Principles and applications for the brain and heart
    • Phelps, M.E.; Mazziotta, J.C.; Schelbert, H.R.; Eds.; Raven Press: New York, Ch 2
    • Young, A.B.; Frey, K.A.; Agranoff, B.W. Positron Emission Tomography and Autoradiography: Principles and Applications for the Brain and Heart. In: In Vitro and In Vivo, Phelps, M.E.; Mazziotta, J.C.; Schelbert, H.R.; Eds.; Raven Press: New York, 1986, Ch 2. pp. 73-111.
    • (1986) Vitro and in Vivo , pp. 73-111
    • Young, A.B.1    Frey, K.A.2    Agranoff, B.W.3
  • 57
    • 0026581855 scopus 로고
    • Protein content of various regions of rat brain and adult and aging human brain
    • Banay-Schwartz, M.; Kenessey, A.; De Guzman, T.; Lajtham, A.; Palkovits, M. Protein content of various regions of rat brain and adult and aging human brain. Age, 1992, 15, 51-54.
    • (1992) Age , vol.15 , pp. 51-54
    • Banay-Schwartz, M.1    Kenessey, A.2    De Guzman, T.3    Lajtham, A.4    Palkovits, M.5
  • 60
    • 79960019023 scopus 로고    scopus 로고
    • Absolute abundances and affinity states of dopamine receptors in mammalian brain: A review
    • Cumming, P. Absolute abundances and affinity states of dopamine receptors in mammalian brain: a review. Synapse, 2011, 65, 892-909.
    • (2011) Synapse , vol.65 , pp. 892-909
    • Cumming, P.1
  • 61
    • 0030610492 scopus 로고    scopus 로고
    • 3H]8-OH-DPAT and demonstration of increased binding in the frontal cortex in schizophrenia
    • 3H]8-OH-DPAT and demonstration of increased binding in the frontal cortex in schizophrenia. Neurochem. Int., 1997, 30, 565-574.
    • (1997) Neurochem. Int. , vol.30 , pp. 565-574
    • Burnett, P.W.J.1    Eastwood, S.L.2    Harrison, P.J.3
  • 67
    • 0025194051 scopus 로고
    • 3H]Ro-15-1788 binding to benzodiazepine receptors in human post mortem brain homogenates
    • 3H]Ro-15-1788 binding to benzodiazepine receptors in human post mortem brain homogenates. J. Neurochem., 1990, 55, 1310-1315.
    • (1990) J. Neurochem. , vol.55 , pp. 1310-1315
    • Kopp, J.1    Hall, H.2    Persson, A.M.3    Sedvall, G.4
  • 74
    • 77956942872 scopus 로고    scopus 로고
    • Pharmacological characterization of the GlyT-1 glycine transporter using two novel radioligands
    • Herdon, H.J.; Roberts, J.C.; Coulton, S.; Porter, R.A. Pharmacological characterization of the GlyT-1 glycine transporter using two novel radioligands. Neuropharmacology, 2010, 59, 558-565.
    • (2010) Neuropharmacology , vol.59 , pp. 558-565
    • Herdon, H.J.1    Roberts, J.C.2    Coulton, S.3    Porter, R.A.4
  • 76
    • 0019956795 scopus 로고
    • Opiate receptor binding sites in human brain
    • Pfeiffer, A.; Pasi, A.; Mehraein, P.; Herz, A. Opiate receptor binding sites in human brain. Brain Res., 1982, 248, 87-96.
    • (1982) Brain Res. , vol.248 , pp. 87-96
    • Pfeiffer, A.1    Pasi, A.2    Mehraein, P.3    Herz, A.4
  • 77
    • 0038689170 scopus 로고    scopus 로고
    • Studies on serotonergic markers in the human hippocampus: Changes in subjects with bipolar disorder
    • Dean, B.; Scarr, E.; Pavey, G.; Copolov, D. Studies on serotonergic markers in the human hippocampus: changes in subjects with bipolar disorder. J. Affect. Disord., 2003, 75, 65-69.
    • (2003) J. Affect. Disord. , vol.75 , pp. 65-69
    • Dean, B.1    Scarr, E.2    Pavey, G.3    Copolov, D.4
  • 80
    • 38949112843 scopus 로고    scopus 로고
    • Kinetic analysis in healthy humans of a novel positron emission tomography radioligand to image the peripheral benzodiazepine receptor, a potential biomarker for inflammation
    • Fujita, M.; Imaizumi, M.; Zoghbi, S.S.; Fujimura, Y.; Farris, A.G.; Suhara, T.; Hong, J.; Pike, V.W.; Innis, R.B. Kinetic analysis in healthy humans of a novel positron emission tomography radioligand to image the peripheral benzodiazepine receptor, a potential biomarker for inflammation. NeuroImage, 2008, 40, 43-52.
    • (2008) NeuroImage , vol.40 , pp. 43-52
    • Fujita, M.1    Imaizumi, M.2    Zoghbi, S.S.3    Fujimura, Y.4    Farris, A.G.5    Suhara, T.6    Hong, J.7    Pike, V.W.8    Innis, R.B.9
  • 81
    • 0027138551 scopus 로고
    • Radioligand binding methods - Practical guide and tips
    • Bylund, D.B.; Teows, M.L. Radioligand binding methods - practical guide and tips. Am. J. Physiol., 1993, 265, L421-L429.
    • (1993) Am. J. Physiol. , vol.265 , pp. L421-L429
    • Bylund, D.B.1    Teows, M.L.2
  • 82
    • 33846032313 scopus 로고    scopus 로고
    • Radioligand development for PET imaging of β-amyloid (Aβ) - Current status
    • Cai, L.; Innis, R.B.; Pike, V.W. Radioligand development for PET imaging of β-amyloid (Aβ) - current status. Curr. Med. Chem., 2007, 14, 19-52.
    • (2007) Curr. Med. Chem. , vol.14 , pp. 19-52
    • Cai, L.1    Innis, R.B.2    Pike, V.W.3
  • 84
    • 37349016705 scopus 로고    scopus 로고
    • 11C]raclopride with ultrahigh specific activity in rat brain determined by homogenate assay and autoradiography
    • 11C]raclopride with ultrahigh specific activity in rat brain determined by homogenate assay and autoradiography. Nucl. Med. Biol., 2008, 35, 19-27.
    • (2008) Nucl. Med. Biol. , vol.35 , pp. 19-27
    • Noguchi, J.1    Zhang, M.-R.2    Yanamoto, K.3    Nakao, R.4    Suzuki, K.5
  • 87
    • 78049403279 scopus 로고    scopus 로고
    • Ligand binding assays at equilibrium: Validation and interpretation
    • Hulme, E.C.; Trevethick, M.A. Ligand binding assays at equilibrium: validation and interpretation. Br. J. Pharmacol., 2010, 161, 1219-1237.
    • (2010) Br. J. Pharmacol. , vol.161 , pp. 1219-1237
    • Hulme, E.C.1    Trevethick, M.A.2
  • 89
    • 78049359776 scopus 로고    scopus 로고
    • 35S]GTPγS and Eu-GTPγS) binding assay for analysis of ligand potency and efficacy at G protein-coupled receptors
    • 35S]GTPγS and Eu-GTPγS) binding assay for analysis of ligand potency and efficacy at G protein-coupled receptors. Br. J. Pharmacol., 2010, 161, 1238-1249.
    • (2010) Br. J. Pharmacol. , vol.161 , pp. 1238-1249
    • Strange, P.G.1
  • 90
  • 93
    • 33749863936 scopus 로고    scopus 로고
    • The quest for Eldorado: Development of radioligands for in vivo imaging of nicotinic acetylcholine receptors in human brain
    • Horti, A.G.; Villemagne, V.L. The quest for Eldorado: development of radioligands for in vivo imaging of nicotinic acetylcholine receptors in human brain. Curr. Radiopharm. Des., 2006, 12, 3877-3900.
    • (2006) Curr. Radiopharm. Des. , vol.12 , pp. 3877-3900
    • Horti, A.G.1    Villemagne, V.L.2
  • 99
    • 70349645989 scopus 로고    scopus 로고
    • A biomathematical modeling approach to central nervous system radioligand discovery and development
    • Guo, Q, Brady, M.; Gunn, R.N. A biomathematical modeling approach to central nervous system radioligand discovery and development. J. Nucl. Med., 2009, 50, 1715-1723.
    • (2009) J. Nucl. Med. , vol.50 , pp. 1715-1723
    • Guo, Q.1    Brady, M.2    Gunn, R.N.3
  • 100
    • 67849083569 scopus 로고    scopus 로고
    • PET radiotracers: Crossing the blood-brain barrier and surviving metabolism
    • Pike, V.W. PET radiotracers: crossing the blood-brain barrier and surviving metabolism. Trends Pharmacol. Sci., 2009, 30, 431-440.
    • (2009) Trends Pharmacol. Sci. , vol.30 , pp. 431-440
    • Pike, V.W.1
  • 102
    • 77958022683 scopus 로고    scopus 로고
    • Development of effective PET and SPECT imaging agents for the serotonin transporter: Has a twenty-year journey reached its destination?
    • Huang, Y.; Zheng, M.-Q.; Gerdes, J.M. Development of effective PET and SPECT imaging agents for the serotonin transporter: has a twenty-year journey reached its destination? Curr. Top. Med. Chem., 2010, 10, 1499-1526.
    • (2010) Curr. Top. Med. Chem. , vol.10 , pp. 1499-1526
    • Huang, Y.1    Zheng, M.-Q.2    Gerdes, J.M.3
  • 103
    • 84862826332 scopus 로고    scopus 로고
    • Selectivity requirements for diagnostic imaging of neurofibrillary lesions in Alzheimer's disease: A simulation study
    • Schafer, K.N.; Kim, S.; Matzavinos, A.; Kuret, J. Selectivity requirements for diagnostic imaging of neurofibrillary lesions in Alzheimer's disease: a simulation study. NeuroImage, 2012, 60, 1724-1733.
    • (2012) NeuroImage , vol.60 , pp. 1724-1733
    • Schafer, K.N.1    Kim, S.2    Matzavinos, A.3    Kuret, J.4
  • 104
    • 79955383737 scopus 로고    scopus 로고
    • N- (4-Cyanotetrahydro-2H-pyran-4-yl) and N-(1-cyanocyclohexyl) derivatives of 1,5-diarylpyrazole-3-carboxamides showing high affinity for 18 kDa translocator protein and/or cannabinoid receptors
    • Donohue, S.R.; Dannals, R.F.; Halldin, C.; Pike, V.W. N- (4-Cyanotetrahydro-2H-pyran-4-yl) and N-(1-cyanocyclohexyl) derivatives of 1,5-diarylpyrazole-3-carboxamides showing high affinity for 18 kDa translocator protein and/or cannabinoid receptors. J. Med. Chem., 2011, 54, 2961-2970.
    • (2011) J. Med. Chem. , vol.54 , pp. 2961-2970
    • Donohue, S.R.1    Dannals, R.F.2    Halldin, C.3    Pike, V.W.4
  • 108
    • 0027238911 scopus 로고
    • Radioligands for PET studies of central benzodiazepine receptors and PK (peripheral benzodiazepine) binding sites - Current status
    • Pike, V.W.; Halldin, C.; Crouzel, C.; Barré, L. Nutt, D.J.; Osman, S.; Shah, F.; Turton, D.R.; Waters, S.L. Radioligands for PET studies of central benzodiazepine receptors and PK (peripheral benzodiazepine) binding sites - current status. Nucl. Med. Biol., 1993, 20, 503-525.
    • (1993) Nucl. Med. Biol. , vol.20 , pp. 503-525
    • Pike, V.W.1    Halldin, C.2    Crouzel, C.3    Barré, L.4    Nutt, D.J.5    Osman, S.6    Shah, F.7    Turton, D.R.8    Waters, S.L.9
  • 109
    • 0344110495 scopus 로고    scopus 로고
    • Molecular structure and stereoelectronic properties of sarmazenil - A weak inverse agonist at the omega modulatory sites (benzodiazepine receptors): Comparison with bretazenil and flumazenil
    • López-Romero, B.; Evrard, G.; Durant, F.; Sevrin, M.; George, P. Molecular structure and stereoelectronic properties of sarmazenil - a weak inverse agonist at the omega modulatory sites (benzodiazepine receptors): comparison with bretazenil and flumazenil. Bioorg. Med. Chem., 1998, 6, 1745-1757.
    • (1998) Bioorg. Med. Chem. , vol.6 , pp. 1745-1757
    • López-Romero, B.1    Evrard, G.2    Durant, F.3    Sevrin, M.4    George, P.5
  • 110
    • 1642495639 scopus 로고    scopus 로고
    • Efficacy as a vector: The relative prevalence and paucity of inverse agonism
    • Kenakin, T. Efficacy as a vector: the relative prevalence and paucity of inverse agonism. Mol. Pharmacol., 2004, 65, 2-11.
    • (2004) Mol. Pharmacol. , vol.65 , pp. 2-11
    • Kenakin, T.1
  • 111
    • 84858236079 scopus 로고    scopus 로고
    • Ensemble of G-protein-coupled receptor active states
    • Park, P.S.-H. Ensemble of G-protein-coupled receptor active states. Curr. Med. Chem., 2012, 19, 1146-1154.
    • (2012) Curr. Med. Chem. , vol.19 , pp. 1146-1154
    • Park, P.S.-H.1
  • 113
    • 0033932559 scopus 로고    scopus 로고
    • 1A receptor agonist-antagonist binding affinity difference as a measure of intrinsic activity in recombinant and native tissue systems
    • 1A receptor agonist-antagonist binding affinity difference as a measure of intrinsic activity in recombinant and native tissue systems. Br. J. Pharmacol., 2000, 130, 1108-1114.
    • (2000) Br. J. Pharmacol. , vol.130 , pp. 1108-1114
    • Watson, J.1    Collin, L.2    Ho, M.3    Riley, G.4    Scott, C.5    Selkirk, J.V.6    Price, G.W.7
  • 115
    • 0032973339 scopus 로고    scopus 로고
    • Relationship between ligand affinities for the cerebellar cannabinoid receptor CB1 and the induction of GDP/GTP exchange
    • Kearn, C.S.; Greenberg, M.J.; Di Camelli, R.; Kurzawa, K.; Hlllard, C.J. Relationship between ligand affinities for the cerebellar cannabinoid receptor CB1 and the induction of GDP/GTP exchange. J. Neurochem., 1999, 72, 2379-2387.
    • (1999) J. Neurochem. , vol.72 , pp. 2379-2387
    • Kearn, C.S.1    Greenberg, M.J.2    Di Camelli, R.3    Kurzawa, K.4    Hlllard, C.J.5
  • 116
  • 117
    • 34447633368 scopus 로고    scopus 로고
    • Conformational complexity of Gprotein-coupled receptors
    • Kobilka, B.K.; Deupi, X. Conformational complexity of Gprotein-coupled receptors. Trends Pharm. Sci., 2007, 28, 397-406.
    • (2007) Trends Pharm. Sci. , vol.28 , pp. 397-406
    • Kobilka, B.K.1    Deupi, X.2
  • 118
    • 66249144426 scopus 로고    scopus 로고
    • The structure and function of G-protein-coupled receptors
    • Rosenbaum, D.M.; Rasmussen, S.G.F.; Kobilka, B.K. The structure and function of G-protein-coupled receptors. Nature, 2009, 459, 356-363.
    • (2009) Nature , vol.459 , pp. 356-363
    • Rosenbaum, D.M.1    Rasmussen, S.G.F.2    Kobilka, B.K.3
  • 119
    • 77958039571 scopus 로고    scopus 로고
    • Energy landscapes as a tool to integrate GPCR structure, dynamics and function
    • Deupi, X.; Kobilka, B.K. Energy landscapes as a tool to integrate GPCR structure, dynamics and function. Physiology, 2010, 25, 293-303.
    • (2010) Physiology , vol.25 , pp. 293-303
    • Deupi, X.1    Kobilka, B.K.2
  • 123
    • 0031772782 scopus 로고    scopus 로고
    • Quantitative analyses of carbonyl-carbon-11 WAY-100635 binding to central 5-hydroxytryptamine-1A receptors in man
    • Farde, L.; Ito, H.; Swahn, C.-G.; Pike, V.W.; Halldin, C. Quantitative analyses of carbonyl-carbon-11 WAY-100635 binding to central 5-hydroxytryptamine-1A receptors in man. J. Nucl. Med., 1998, 39, 1965-1971.
    • (1998) J. Nucl. Med. , vol.39 , pp. 1965-1971
    • Farde, L.1    Ito, H.2    Swahn, C.-G.3    Pike, V.W.4    Halldin, C.5
  • 138
    • 81555213468 scopus 로고    scopus 로고
    • Dopamine agonist radioligand binds to both D2high and D2low receptors, explaining why alterations in D2high are not detected in human brain scans
    • Seeman, P. Dopamine agonist radioligand binds to both D2high and D2low receptors, explaining why alterations in D2high are not detected in human brain scans. Synapse, 2012, 66, 88-93.
    • (2012) Synapse , vol.66 , pp. 88-93
    • Seeman, P.1
  • 139
    • 77649319236 scopus 로고
    • Multicompartmental analysis of C-11 carfentanil binding to opiate receptors in man by positron emission tomography
    • Frost, J.J.; Douglass, K.; Mayberg, H.; Dannals, R.F.; Links, J.; Wilson, A.; Ravert, H.; Wagner, H.N. Multicompartmental analysis of C-11 carfentanil binding to opiate receptors in man by positron emission tomography. J. Nucl. Med., 1986, 27, 1027-1027.
    • (1986) J. Nucl. Med. , vol.27 , pp. 1027
    • Frost, J.J.1    Douglass, K.2    Mayberg, H.3    Dannals, R.F.4    Links, J.5    Wilson, A.6    Ravert, H.7    Wagner, H.N.8
  • 142
    • 84888040704 scopus 로고    scopus 로고
    • Development of allosteric modulators of GPCRs for treatment
    • Highfield Nickols, H.; Conn, P.J. Development of allosteric modulators of GPCRs for treatment. Neurobiol. Dis., 2014, 61, 55-71.
    • (2014) Neurobiol. Dis. , vol.61 , pp. 55-71
    • Highfield Nickols, H.1    Conn, P.J.2
  • 144
    • 77957989521 scopus 로고    scopus 로고
    • Radioligands for the PET imaging of metabotropic glutamate receptor subtype 5 (mGluR5)
    • Mu, L.; Schubiger, P.A.; Ametamey, S.M. Radioligands for the PET imaging of metabotropic glutamate receptor subtype 5 (mGluR5). Curr. Top. Med. Chem., 2010, 10, 1558-1568.
    • (2010) Curr. Top. Med. Chem. , vol.10 , pp. 1558-1568
    • Mu, L.1    Schubiger, P.A.2    Ametamey, S.M.3
  • 165
    • 34447520294 scopus 로고    scopus 로고
    • 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl) benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography
    • 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl) benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography. J. Med. Chem., 2007, 50, 3256-3266.
    • (2007) J. Med. Chem. , vol.50 , pp. 3256-3266
    • Siméon, F.G.1    Brown, A.K.2    Zoghbi, S.S.3    Patterson, V.M.4    Innis, R.B.5    Pike, V.W.6
  • 169
    • 0032410164 scopus 로고    scopus 로고
    • Estimation of blood-brain barrier crossing of drugs using molecular size and shape, and Hbonding descriptors
    • van de Waterbeemd, H.; Camenish, G.; Folkers, G.; Chretien, J.R.; Raevsky, O.A. Estimation of blood-brain barrier crossing of drugs using molecular size and shape, and Hbonding descriptors. J. Drug Targeting, 1998, 6, 151-165.
    • (1998) J. Drug Targeting , vol.6 , pp. 151-165
    • Van-De-Waterbeemd, H.1    Camenish, G.2    Folkers, G.3    Chretien, J.R.4    Raevsky, O.A.5
  • 170
    • 0031024171 scopus 로고    scopus 로고
    • Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
    • Lipinski, C.A.; Lombardo, F.; Dominy, B.W.; Feeney, P.J. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv. Drug Deliv. Rev., 1997, 23, 3-26.
    • (1997) Adv. Drug Deliv. Rev. , vol.23 , pp. 3-26
    • Lipinski, C.A.1    Lombardo, F.2    Dominy, B.W.3    Feeney, P.J.4
  • 171
    • 0032714220 scopus 로고    scopus 로고
    • Polar molecular surface as a dominating determinant for oral absorption and brain penetration of drugs
    • Kelder, J.; Grootenhuis, P.D.J.; Byada, D.M.; Delbressine, L.P.C.; Ploemen, J.P. Polar molecular surface as a dominating determinant for oral absorption and brain penetration of drugs. Pharm. Res., 1999, 16, 1514-1519.
    • (1999) Pharm. Res. , vol.16 , pp. 1514-1519
    • Kelder, J.1    Grootenhuis, P.D.J.2    Byada, D.M.3    Delbressine, L.P.C.4    Ploemen, J.P.5
  • 172
    • 0037204545 scopus 로고    scopus 로고
    • Computational approaches to the prediction of the blood-brain distribution
    • Norinder, U.; Haeberlein, M. Computational approaches to the prediction of the blood-brain distribution. Adv. Drug Delivery Rev., 2002, 54, 291-313.
    • (2002) Adv. Drug Delivery Rev. , vol.54 , pp. 291-313
    • Norinder, U.1    Haeberlein, M.2
  • 173
    • 33845937770 scopus 로고    scopus 로고
    • Structure-brain exposure relationships
    • Hitchock, S.A.; Pennington, L.D. Structure-brain exposure relationships. J. Med. Chem., 2006, 49, 7559-7583.
    • (2006) J. Med. Chem. , vol.49 , pp. 7559-7583
    • Hitchock, S.A.1    Pennington, L.D.2
  • 174
    • 39749181550 scopus 로고    scopus 로고
    • Generation of a set of simple, interpretable ADMET rules of thumb
    • Gleeson, M.P. Generation of a set of simple, interpretable ADMET rules of thumb. J. Med. Chem., 2008, 51, 817-834.
    • (2008) J. Med. Chem. , vol.51 , pp. 817-834
    • Gleeson, M.P.1
  • 176
    • 84855907412 scopus 로고    scopus 로고
    • On quantitative relationships between drug-like compound lipophilicity and plasma free fraction in monkey and human
    • Zoghbi, S.S.; Anderson, K.B.; Jenko, K.J.; Luckenbaugh, D.A.; Innis, R.B.; Pike, V.W. On quantitative relationships between drug-like compound lipophilicity and plasma free fraction in monkey and human. J. Pharm. Sci., 2012, 101, 1028-1039.
    • (2012) J. Pharm. Sci. , vol.101 , pp. 1028-1039
    • Zoghbi, S.S.1    Anderson, K.B.2    Jenko, K.J.3    Luckenbaugh, D.A.4    Innis, R.B.5    Pike, V.W.6
  • 178
    • 0344121272 scopus 로고    scopus 로고
    • Determination of lipophilicity and its use as a predictor of blood-brain barrier penetration of molecular imaging targets
    • Waterhouse, R.N. Determination of lipophilicity and its use as a predictor of blood-brain barrier penetration of molecular imaging targets. Mol. Imaging Biol., 2003, 5, 376-389.
    • (2003) Mol. Imaging Biol. , vol.5 , pp. 376-389
    • Waterhouse, R.N.1
  • 179
    • 84925854124 scopus 로고    scopus 로고
    • CNS drug design: Balancing physicochemical properties for optimal brain exposure
    • Rankovic, Z. CNS drug design: balancing physicochemical properties for optimal brain exposure. J. Med. Chem., 2015, 58, 2584-2608.
    • (2015) J. Med. Chem. , vol.58 , pp. 2584-2608
    • Rankovic, Z.1
  • 180
    • 0034609833 scopus 로고    scopus 로고
    • Fast calculation of molecular polar surface area as a sum of fragment-based contributions and its application to the prediction of drug transport properties
    • Ertl, P.; Rohde, B.; Selzer, P. Fast calculation of molecular polar surface area as a sum of fragment-based contributions and its application to the prediction of drug transport properties. J. Med. Chem., 2000, 43, 3714-3717.
    • (2000) J. Med. Chem. , vol.43 , pp. 3714-3717
    • Ertl, P.1    Rohde, B.2    Selzer, P.3
  • 181
    • 0032811868 scopus 로고    scopus 로고
    • Rapid calculation of polar molecular surface area and its application to the prediction of transport phenomena. 2. Prediction of blood-brain barrier penetration
    • Clark, D.E. Rapid calculation of polar molecular surface area and its application to the prediction of transport phenomena. 2. Prediction of blood-brain barrier penetration. J. Pharm. Sci., 1999, 88, 815-821.
    • (1999) J. Pharm. Sci. , vol.88 , pp. 815-821
    • Clark, D.E.1
  • 182
    • 33646849102 scopus 로고    scopus 로고
    • Computational approaches to the prediction of blood-brain barrier permeability: A comparative analysis of central nervous system drugs versus secretase inhibitors for Alzheimer's disease
    • Rishton, G.M.; La Bonte, K.; Williams, A.J.; Kassa, K.; Kolanov, E. Computational approaches to the prediction of blood-brain barrier permeability: a comparative analysis of central nervous system drugs versus secretase inhibitors for Alzheimer's disease. Curr. Opin. Drug Disc. Dev., 2006, 9, 303-313.
    • (2006) Curr. Opin. Drug Disc. Dev. , vol.9 , pp. 303-313
    • Rishton, G.M.1    La Bonte, K.2    Williams, A.J.3    Kassa, K.4    Kolanov, E.5
  • 183
    • 33749510509 scopus 로고    scopus 로고
    • In silico prediction of blood-brain barrier permeation using the calculated molecular crosssectional area as main parameter
    • Gerebtzoff, G.; Seelig, A. In silico prediction of blood-brain barrier permeation using the calculated molecular crosssectional area as main parameter. J. Chem. Inf. Model, 2006, 46, 2638-2650.
    • (2006) J. Chem. Inf. Model , vol.46 , pp. 2638-2650
    • Gerebtzoff, G.1    Seelig, A.2
  • 184
    • 1542426103 scopus 로고    scopus 로고
    • Blood-brain barrier permeation models: Discriminating between potential CNS and non-CNS drugs including P-glycoprotein substrates
    • Adenot, M.; Lahana, R. Blood-brain barrier permeation models: discriminating between potential CNS and non-CNS drugs including P-glycoprotein substrates. J. Comput. Inf. Comput. Sci., 2004, 44, 239-248.
    • (2004) J. Comput. Inf. Comput. Sci. , vol.44 , pp. 239-248
    • Adenot, M.1    Lahana, R.2
  • 186
    • 84875485383 scopus 로고    scopus 로고
    • Confounding parameters in preclinical assessment of blood-brain barrier permeation: An overview with emphasis on species differences and effect of disease states
    • Deo, A.K.; Theil, F.P.; Nicolas, J.M. Confounding parameters in preclinical assessment of blood-brain barrier permeation: an overview with emphasis on species differences and effect of disease states. Mol. Pharmaceutics, 2013, 10, 1581-1595.
    • (2013) Mol. Pharmaceutics , vol.10 , pp. 1581-1595
    • Deo, A.K.1    Theil, F.P.2    Nicolas, J.M.3
  • 187
    • 84978032137 scopus 로고    scopus 로고
    • Last accessed 01/19
    • ACD/Labs data sheet. Available from: http://www.acdlabs.com/download/docs/datasheets/datasheet-bbb.pdf. Last accessed 01/19/2016
    • (2016) ACD/Labs Data Sheet
  • 188
    • 84925493662 scopus 로고    scopus 로고
    • Drug transporters in the central nervous system
    • Stieger, B.; Gao, B. Drug transporters in the central nervous system. Clin. Pharmacokinet., 2015, 54, 225-242.
    • (2015) Clin. Pharmacokinet. , vol.54 , pp. 225-242
    • Stieger, B.1    Gao, B.2
  • 189
    • 33644691806 scopus 로고    scopus 로고
    • Comparison of species differences of P-glycoproteins in beagle dog, rhesus monkey, and human using ATPase activity assays
    • Xia, C.Q.; Xiao, G.; Liu, N.; Pimprale, S.; Fox, L.; Patten, C.J.; Crespi, C.L.; Miwa, G.; Gan, L.S. Comparison of species differences of P-glycoproteins in beagle dog, rhesus monkey, and human using ATPase activity assays. Mol. Pharm., 2006, 3, 78-86.
    • (2006) Mol. Pharm. , vol.3 , pp. 78-86
    • Xia, C.Q.1    Xiao, G.2    Liu, N.3    Pimprale, S.4    Fox, L.5    Patten, C.J.6    Crespi, C.L.7    Miwa, G.8    Gan, L.S.9
  • 190
    • 61449118888 scopus 로고    scopus 로고
    • Species differences in blood-brain barrier transport of three positron emission tomography radioligands with emphasis on P-glycoprotein transport
    • Syvänen, S.; Lindhe, O.; Palner, M.; Kornum, B.R.; Rahman, O.; Långström, B.; Knudsen, G.M.; Hammarlund-Udenaes, M. Species differences in blood-brain barrier transport of three positron emission tomography radioligands with emphasis on P-glycoprotein transport. Drug Metab. Dispos., 2009, 37, 635-643.
    • (2009) Drug Metab. Dispos. , vol.37 , pp. 635-643
    • Syvänen, S.1    Lindhe, O.2    Palner, M.3    Kornum, B.R.4    Rahman, O.5    Långström, B.6    Knudsen, G.M.7    Hammarlund-Udenaes, M.8
  • 191
    • 0034051677 scopus 로고    scopus 로고
    • Enhanced cerebral uptake of receptor ligands by modulation of P-glycoprotein function in the bloodbrain-barrier
    • Doze, P.; van Waarde, A.; Elsinga, P.H.; Hendrikse, N.H.; Vaalburg, W. Enhanced cerebral uptake of receptor ligands by modulation of P-glycoprotein function in the bloodbrain-barrier. Synapse, 2000, 36, 66-74.
    • (2000) Synapse , vol.36 , pp. 66-74
    • Doze, P.1    Van Waarde, A.2    Elsinga, P.H.3    Hendrikse, N.H.4    Vaalburg, W.5
  • 193
    • 25144446459 scopus 로고    scopus 로고
    • Positron emission tomography studies on binding of central nervous system drugs and P-glycoprotein function in the rodent brain
    • Elsinga, P.H.; Hendrikse, N.H.; Bart, J.; van Waarde, A.; Vaalburg, W. Positron emission tomography studies on binding of central nervous system drugs and P-glycoprotein function in the rodent brain. Mol. Imaging Biol., 2005, 7, 37-44
    • (2005) Mol. Imaging Biol. , vol.7 , pp. 37-44
    • Elsinga, P.H.1    Hendrikse, N.H.2    Bart, J.3    Van Waarde, A.4    Vaalburg, W.5
  • 201
    • 33847275232 scopus 로고    scopus 로고
    • In vivo evaluation of P-glycoprotein modulation of 8 PET radioligands used clinically
    • Ishiwata, K.; Kawamura, K.; Yanai, K.; Hendrikse, N.H. In vivo evaluation of P-glycoprotein modulation of 8 PET radioligands used clinically. J. Nucl. Med., 2007, 48, 81-87.
    • (2007) J. Nucl. Med. , vol.48 , pp. 81-87
    • Ishiwata, K.1    Kawamura, K.2    Yanai, K.3    Hendrikse, N.H.4
  • 207
    • 84920428844 scopus 로고    scopus 로고
    • Increased permeability-glycoprotein inhibition at the human blood-brain barrier can be safely achieved by performing PET during peak plasma concentrations of tariquidar
    • Kreisl, W.C.; Bhatia, R; Morse, C.L.; Woock, A.E.; Zoghbi, S.S.; Shetty, H.U.; Pike, V.W.; Innis, R.B. Increased permeability-glycoprotein inhibition at the human blood-brain barrier can be safely achieved by performing PET during peak plasma concentrations of tariquidar J. Nucl. Med., 2015, 56, 82-87.
    • (2015) J. Nucl. Med. , vol.56 , pp. 82-87
    • Kreisl, W.C.1    Bhatia, R.2    Morse, C.L.3    Woock, A.E.4    Zoghbi, S.S.5    Shetty, H.U.6    Pike, V.W.7    Innis, R.B.8
  • 208
    • 41549102797 scopus 로고    scopus 로고
    • Computational models for prediction of interactions with ABC-transporters
    • Ecker, G.F.; Stockner, T.; Chiba, P. Computational models for prediction of interactions with ABC-transporters. Drug Discov. Today, 2008, 13, 311-317.
    • (2008) Drug Discov. Today , vol.13 , pp. 311-317
    • Ecker, G.F.1    Stockner, T.2    Chiba, P.3
  • 209
    • 77952654824 scopus 로고    scopus 로고
    • Ensemble rule-based classification of substrates of the human ABC-transporter ABCB1 using simple physiochemical descriptors
    • Demel, M.A.; Kraemer O.; Ettmayer, P.; Haaksma, E.; Ecker, G.F. Ensemble rule-based classification of substrates of the human ABC-transporter ABCB1 using simple physiochemical descriptors. Mol. Inf., 2010, 29, 233-242.
    • (2010) Mol. Inf. , vol.29 , pp. 233-242
    • Demel, M.A.1    Kraemer, O.2    Ettmayer, P.3    Haaksma, E.4    Ecker, G.F.5
  • 210
    • 0032518454 scopus 로고    scopus 로고
    • A general pattern for substrate recognition by Pglycoprotein
    • Seelig, A. A general pattern for substrate recognition by Pglycoprotein. Eur. J. Biochem., 1998, 251, 252-261.
    • (1998) Eur. J. Biochem. , vol.251 , pp. 252-261
    • Seelig, A.1
  • 211
    • 14544269934 scopus 로고    scopus 로고
    • Inhibitors of multidrug efflux transporters: Their membrane and protein interactions
    • Seelig, A.; Gatlik-Landwojtowicz, E. Inhibitors of multidrug efflux transporters: their membrane and protein interactions. Mini-Rev. Med. Chem., 2005, 5, 135-151.
    • (2005) Mini-Rev. Med. Chem. , vol.5 , pp. 135-151
    • Seelig, A.1    Gatlik-Landwojtowicz, E.2
  • 212
    • 84862296187 scopus 로고    scopus 로고
    • Structural modifications that alter the Pglycoprotein efflux properties of compounds
    • Hitchcock, S.A. Structural modifications that alter the Pglycoprotein efflux properties of compounds. J. Med. Chem., 2012, 55, 4877-4895.
    • (2012) J. Med. Chem. , vol.55 , pp. 4877-4895
    • Hitchcock, S.A.1
  • 213
    • 84875761790 scopus 로고    scopus 로고
    • Integration of in silico and in vitro tools for scaffold optimization during drug discovery: Predicting P-glycoprotein efflux
    • Desai, P.V.; Sawada, G.A.; Watson, I.A.; Raub, T.J. Integration of in silico and in vitro tools for scaffold optimization during drug discovery: predicting P-glycoprotein efflux. Mol. Pharm., 2013, 10, 1249-1261.
    • (2013) Mol. Pharm. , vol.10 , pp. 1249-1261
    • Desai, P.V.1    Sawada, G.A.2    Watson, I.A.3    Raub, T.J.4
  • 214
  • 215
    • 0036874825 scopus 로고    scopus 로고
    • Influence of nonspecific brain and plasma binding on CNS exposure: Implications for rational drug discovery
    • Kalvass, J.C.; Maurer, T.S., Influence of nonspecific brain and plasma binding on CNS exposure: implications for rational drug discovery. Biopharm. Drug Dispos. 2002, 23, 327-338.
    • (2002) Biopharm. Drug Dispos. , vol.23 , pp. 327-338
    • Kalvass, J.C.1    Maurer, T.S.2
  • 216
    • 33644756715 scopus 로고    scopus 로고
    • Improving the in vitro prediction of the in vivo central nervous system penetration: Integrating permeability, P-glycoprotein efflux, and free fractions in blood and brain
    • Summerfield, S.G.; Stevens, A.J.; Cutler, L., del Carmen, O.M.; Hammond, P.; Tang, S.P.; Hersey, A. Spaldinh, D.J.; Jeffrey, P. Improving the in vitro prediction of the in vivo central nervous system penetration: integrating permeability, P-glycoprotein efflux, and free fractions in blood and brain. J. Pharmacol. Exp. Ther., 2006, 316, 1282-1290.
    • (2006) J. Pharmacol. Exp. Ther. , vol.316 , pp. 1282-1290
    • Summerfield, S.G.1    Stevens, A.J.2    Cutler, L.3    Del Carmen, O.M.4    Hammond, P.5    Tang, S.P.6    Hersey, A.7    Spaldinh, D.J.8    Jeffrey, P.9
  • 217
    • 0028289554 scopus 로고
    • Evaluation of ultrafiltration for the freefraction determination of single photon emission computed tomography (SPECT) radiotracers: Beta-CIT, IBF, and iomazenil
    • Gandelman, M.S.; Baldwin, R.M.; Zoghbi, S.S.; Zea-Ponce, Y.; Innis R.B. Evaluation of ultrafiltration for the freefraction determination of single photon emission computed tomography (SPECT) radiotracers: beta-CIT, IBF, and iomazenil. J. Pharm. Sci., 1994, 83, 1014-1019.
    • (1994) J. Pharm. Sci. , vol.83 , pp. 1014-1019
    • Gandelman, M.S.1    Baldwin, R.M.2    Zoghbi, S.S.3    Zea-Ponce, Y.4    Innis, R.B.5
  • 218
    • 33846230530 scopus 로고    scopus 로고
    • Plasma protein binding affinity and its relationship to molecular structure: And in silico analysis
    • Gleeson, M.P. Plasma protein binding affinity and its relationship to molecular structure: and in silico analysis. J. Med. Chem., 2007, 50, 101-112.
    • (2007) J. Med. Chem. , vol.50 , pp. 101-112
    • Gleeson, M.P.1
  • 223
    • 84942241944 scopus 로고    scopus 로고
    • Label-free assay for the assessment of nonspecific binding of positron emission tomography tracer candidates
    • Assmus, F.; Seelig, A.; Gobbi L.; Borroni E.; Glaaentzlin, P.; Fischer, H. Label-free assay for the assessment of nonspecific binding of positron emission tomography tracer candidates. Eur. J. Pharm. Sci., 2015, 79, 27-35.
    • (2015) Eur. J. Pharm. Sci. , vol.79 , pp. 27-35
    • Assmus, F.1    Seelig, A.2    Gobbi, L.3    Borroni, E.4    Glaaentzlin, P.5    Fischer, H.6
  • 224
    • 52649180981 scopus 로고    scopus 로고
    • Ab initio computational study of positron emission tomography ligands interacting with lipid molecule for the prediction of nonspecific binding
    • Rosso, L.; Gee, A.D.; Gould, I.R. Ab initio computational study of positron emission tomography ligands interacting with lipid molecule for the prediction of nonspecific binding. J. Comput. Chem., 2008, 29, 2397-2405.
    • (2008) J. Comput. Chem. , vol.29 , pp. 2397-2405
    • Rosso, L.1    Gee, A.D.2    Gould, I.R.3
  • 260
    • 2942622711 scopus 로고    scopus 로고
    • 2 receptor density and affinity in the human brain using PET
    • 2 receptor density and affinity in the human brain using PET. Neuroimage, 2004, 22, 794-803.
    • (2004) Neuroimage , vol.22 , pp. 794-803
    • Olsson, H.1    Halldin, C.2    Farde, L.3
  • 289
    • 0011053116 scopus 로고    scopus 로고
    • Welch, M.J.; Redvanly, C.S. Eds.; Wiley & Sons Ltd: Chichester: Ch: 75
    • Ferrieri, R.A. In: Handbook of Radiopharmaceuticals. Welch, M.J.; Redvanly, C.S. Eds.; Wiley & Sons Ltd: Chichester: 2003, Ch: 75. pp. 229-282.
    • (2003) Handbook of Radiopharmaceuticals , pp. 229-282
    • Ferrieri, R.A.1
  • 292
    • 84978097844 scopus 로고    scopus 로고
    • Scintomics Print Media and Publishing: Fürstenfeldbruck, Ch. 2
    • Henriksen, G. In: Munich Molecular Imaging Handbook Series. Vol. 1. Scintomics Print Media and Publishing: Fürstenfeldbruck, 2010; Ch. 2, pp. 75-101.
    • (2010) Munich Molecular Imaging Handbook Series , vol.1 , pp. 75-101
    • Henriksen, G.1
  • 294
    • 4043075234 scopus 로고    scopus 로고
    • Welch, M.J.; Redvanly, C.S., Eds.; Wiley & Sons Ltd: Chichester; Ch 6
    • Snyder, S.E.; Kilbourn, M.R. In: Handbook of Radiopharmaceuticals. Welch, M.J.; Redvanly, C.S., Eds.; Wiley & Sons Ltd: Chichester; 2003, Ch 6. pp. 195-227.
    • (2003) Handbook of Radiopharmaceuticals , pp. 195-227
    • Snyder, S.E.1    Kilbourn, M.R.2
  • 295
    • 36749084187 scopus 로고    scopus 로고
    • Recent developments and trends in F-18-radiochemistry: Syntheses and applications
    • Schirrmacher, R.; Wangler, C.; Schirrmacher, E. Recent developments and trends in F-18-radiochemistry: syntheses and applications. Mini-Rev. Org. Chem., 2007, 4, 317-329.
    • (2007) Mini-Rev. Org. Chem. , vol.4 , pp. 317-329
    • Schirrmacher, R.1    Wangler, C.2    Schirrmacher, E.3
  • 298
    • 84897448248 scopus 로고    scopus 로고
    • Radiosyntheses using fluorine-18: The art and science of late stage fluorination
    • Cole, E.; Stewart, M.; Littich, R.; Hoareau, R.; Scott, P.J.H. Radiosyntheses using fluorine-18: the art and science of late stage fluorination. Curr. Topics Med. Chem., 2014, 14, 875-900.
    • (2014) Curr. Topics Med. Chem. , vol.14 , pp. 875-900
    • Cole, E.1    Stewart, M.2    Littich, R.3    Hoareau, R.4    Scott, P.J.H.5
  • 300
    • 84921456136 scopus 로고    scopus 로고
    • Fluorine-18 radiochemistry, labeling strategies and synthetic routes
    • Jacobson, O.; Kiesewetter, D.O.; Chen, X. Fluorine-18 radiochemistry, labeling strategies and synthetic routes. Bioconjugate Chem., 2015, 26, 1-18.
    • (2015) Bioconjugate Chem. , vol.26 , pp. 1-18
    • Jacobson, O.1    Kiesewetter, D.O.2    Chen, X.3
  • 302
    • 0031951911 scopus 로고    scopus 로고
    • Pharmacological constraints associated with positron emission tomographic scanning of small laboratory animals
    • Hume, S.P.; Gunn, R.N.; Jones, T. Pharmacological constraints associated with positron emission tomographic scanning of small laboratory animals. Eur. J. Nucl. Med., 1998, 25, 173-176.
    • (1998) Eur. J. Nucl. Med. , vol.25 , pp. 173-176
    • Hume, S.P.1    Gunn, R.N.2    Jones, T.3
  • 303
    • 3042789514 scopus 로고    scopus 로고
    • Experiment assessment of mass effects in the rat: Implications for small animal PET imaging
    • Jagoda, E.M.; Vaquero, J.J.; Seidel, J.; Green, M.V.; Eckelman, W.C. Experiment assessment of mass effects in the rat: implications for small animal PET imaging. Nucl. Med. Biol., 2004, 31, 771-779.
    • (2004) Nucl. Med. Biol. , vol.31 , pp. 771-779
    • Jagoda, E.M.1    Vaquero, J.J.2    Seidel, J.3    Green, M.V.4    Eckelman, W.C.5
  • 304
    • 84909452381 scopus 로고
    • 11C-carbon dioxide from a nitrogen gas target
    • 11C-carbon dioxide from a nitrogen gas target. J. Nucl. Med., 1972, 13, 429-430.
    • (1972) J. Nucl. Med. , vol.13 , pp. 429-430
    • Finn, R.D.1    Wolf, A.P.2
  • 306
    • 84875272121 scopus 로고    scopus 로고
    • A historical perspective on the specific activity of radiopharmaceuticals: What have we learned in the 35 years of the ISRC
    • Lapi, S.E.; Welch, M.J. A historical perspective on the specific activity of radiopharmaceuticals: what have we learned in the 35 years of the ISRC. Nucl. Med. Biol., 2013, 40, 314-320.
    • (2013) Nucl. Med. Biol. , vol.40 , pp. 314-320
    • Lapi, S.E.1    Welch, M.J.2
  • 307
    • 0033830739 scopus 로고    scopus 로고
    • 2 gas target: Effect of irradiation dose, irradiation history, oxygen content and beam energy
    • 2 gas target: effect of irradiation dose, irradiation history, oxygen content and beam energy. Radiochim. Acta, 2000, 88, 211-215.
    • (2000) Radiochim. Acta , vol.88 , pp. 211-215
    • Suzuki, K.1    Yamazaki, T.2    Sasaki, M.3    Kubodera, A.4
  • 322
    • 56349083698 scopus 로고    scopus 로고
    • 3I synthesized by the wet method; Main sources of noradioactive carbon
    • 3I synthesized by the wet method; main sources of noradioactive carbon. Appl. Radiat. Isot., 2008, 67, 111-114.
    • (2008) Appl. Radiat. Isot. , vol.67 , pp. 111-114
    • Gomez-Vallejo, V.1    Llop, J.2
  • 324
    • 0031079411 scopus 로고    scopus 로고
    • Synthesis of C-11 iodomethane by iodination of C-11 methane
    • Larsen, P.; Ulin, J.; Dahlstrom, K.; Jensen, M. Synthesis of C-11 iodomethane by iodination of C-11 methane. Appl. Radiat. Isot., 1997, 48, 153-157.
    • (1997) Appl. Radiat. Isot. , vol.48 , pp. 153-157
    • Larsen, P.1    Ulin, J.2    Dahlstrom, K.3    Jensen, M.4
  • 325
    • 39749117425 scopus 로고    scopus 로고
    • 3I through gas phase iodination reaction using a TRACERlab FX(C) synthesis module
    • 3I through gas phase iodination reaction using a TRACERlab FX(C) synthesis module. Appl. Radiat. Isot., 2008, 66, 482-488.
    • (2008) Appl. Radiat. Isot. , vol.66 , pp. 482-488
    • Kniess, T.1    Rode, K.2    Wuest, F.3
  • 333
    • 0022384528 scopus 로고
    • The preparation of carbon- 11 labelled diprenorphine: A new radioligand for the study of the opiate receptor system in vivo
    • Luthra, S.K.; Pike, V.W.; Brady F. The preparation of carbon- 11 labelled diprenorphine: a new radioligand for the study of the opiate receptor system in vivo. J. Chem. Soc.; Chem. Commun., 1985, 1423-1425.
    • (1985) J. Chem. Soc.; Chem. Commun. , pp. 1423-1425
    • Luthra, S.K.1    Pike, V.W.2    Brady, F.3
  • 343
    • 35748953087 scopus 로고    scopus 로고
    • 11C]Carbon monoxide, a versatile and useful precursor in labelling chemistry for PET ligand development
    • 11C]Carbon monoxide, a versatile and useful precursor in labelling chemistry for PET ligand development. J. Labelled Comp. Radiopharm., 2007, 50, 794-810.
    • (2007) J. Labelled Comp. Radiopharm. , vol.50 , pp. 794-810
    • Långström, B.1    Itsenko, O.2    Rahman, O.3
  • 345
    • 84925659211 scopus 로고    scopus 로고
    • 11C]Carbon monoxide in labeling chemistry and positron emission tomography tracer development: Scope and limitations
    • 11C]Carbon monoxide in labeling chemistry and positron emission tomography tracer development: scope and limitations. J. Labelled Comp. Radiopharm., 2015, 58, 86-98.
    • (2015) J. Labelled Comp. Radiopharm. , vol.58 , pp. 86-98
    • Rahman, O.1
  • 349
    • 84929359199 scopus 로고    scopus 로고
    • Total cyanide mass measurement with micro-ion selective electrode for determination of specific activity of carbon-11 cyanide
    • Shea, C.; Alexoff, D.L.; Kim, D.; Hoque, R.; Schueller, M.J.; Fowler, J.S.; Qu, W. Total cyanide mass measurement with micro-ion selective electrode for determination of specific activity of carbon-11 cyanide. Appl. Radiat. Isot., 2015, 102, 48-54.
    • (2015) Appl. Radiat. Isot. , vol.102 , pp. 48-54
    • Shea, C.1    Alexoff, D.L.2    Kim, D.3    Hoque, R.4    Schueller, M.J.5    Fowler, J.S.6    Qu, W.7
  • 356
    • 0023234591 scopus 로고
    • A new synthesis of carbon-11 labeled phosgene
    • Landais, P.; Crouzel, C. A new synthesis of carbon-11 labeled phosgene. Appl. Radiat. Isot., 1987, 38, 297-300.
    • (1987) Appl. Radiat. Isot. , vol.38 , pp. 297-300
    • Landais, P.1    Crouzel, C.2
  • 359
    • 77958009659 scopus 로고    scopus 로고
    • 11C]Phosgene: A versatile reagent for radioactive carbonyl insertion into medicinal radiotracers for positron emission tomography
    • 11C]Phosgene: a versatile reagent for radioactive carbonyl insertion into medicinal radiotracers for positron emission tomography. Curr. Top. Med. Chem., 2010, 10, 1680-1700.
    • (2010) Curr. Top. Med. Chem. , vol.10 , pp. 1680-1700
    • Roeda, D.1    Dollé, F.2
  • 364
    • 73249138886 scopus 로고    scopus 로고
    • Teflon radiolysis as the major source of carrier in fluorine-18
    • Berridge, M.S.; Apana, S.M.; Hersch, J.M. Teflon radiolysis as the major source of carrier in fluorine-18. J. Label. Compd. Radiopharm., 2009, 52, 543-548.
    • (2009) J. Label. Compd. Radiopharm. , vol.52 , pp. 543-548
    • Berridge, M.S.1    Apana, S.M.2    Hersch, J.M.3
  • 365
    • 0028964653 scopus 로고
    • 18F]fluoropropyl)- 2,3-dimethoxybenzamide as an improved dopamine D-2 receptor tracer
    • 18F]fluoropropyl)- 2,3-dimethoxybenzamide as an improved dopamine D-2 receptor tracer. Nucl. Med. Biol., 1995, 22, 283-296.
    • (1995) Nucl. Med. Biol. , vol.22 , pp. 283-296
    • Mukherjee, J.1    Yang, Z.Y.2    Das, M.K.3    Brown, T.4
  • 367
    • 24944515476 scopus 로고    scopus 로고
    • Fluorine-18-labelled fluoropyridines: Advances in radiopharmaceutical design
    • Dollé, F. Fluorine-18-labelled fluoropyridines: advances in radiopharmaceutical design. Curr. Pharm. Des., 2005, 11, 3221-3235.
    • (2005) Curr. Pharm. Des. , vol.11 , pp. 3221-3235
    • Dollé, F.1
  • 372
    • 84904189361 scopus 로고    scopus 로고
    • Spirocyclic hypervalent iodine(III)-mediated radiofluorination of non-activated and hindered aromatics
    • Rotstein, B.H.; Stephenson, N.A.; Vasdev, N.; Liang, S.H. Spirocyclic hypervalent iodine(III)-mediated radiofluorination of non-activated and hindered aromatics. Nat. Commun., 2014, 5, 1-7.
    • (2014) Nat. Commun. , vol.5 , pp. 1-7
    • Rotstein, B.H.1    Stephenson, N.A.2    Vasdev, N.3    Liang, S.H.4
  • 373
    • 84880797120 scopus 로고    scopus 로고
    • Applications of iodonium salts and iodonium ylides as precursors for nucleophilic fluorination in positron emission tomography
    • Yusubov, M.S.; Svitch, D.Y.; Larkina, M.S.; Zhdankin, V.V. Applications of iodonium salts and iodonium ylides as precursors for nucleophilic fluorination in positron emission tomography. Arkivoc, 2013 (i) 364-395.
    • (2013) Arkivoc , vol.1 , pp. 364-395
    • Yusubov, M.S.1    Svitch, D.Y.2    Larkina, M.S.3    Zhdankin, V.V.4
  • 376
    • 84939892889 scopus 로고    scopus 로고
    • 18F]flumazenil from iodonium tosylate using a sample pretreatment method: A 2.5-year production report
    • 18F]flumazenil from iodonium tosylate using a sample pretreatment method: a 2.5-year production report. Mol. Imaging Biol. 2014, 16, 619-625.
    • (2014) Mol. Imaging Biol. , vol.16 , pp. 619-625
    • Moon, B.S.1    Park, J.H.2    Lee, H.J.3    Lee, B.C.4    Kim, S.E.5
  • 381
    • 36249019306 scopus 로고    scopus 로고
    • 18F]Fluoroalkyl agents: Synthesis, reactivity and application for development of PET ligands in molecular imaging
    • 18F]Fluoroalkyl agents: synthesis, reactivity and application for development of PET ligands in molecular imaging. Curr. Top. Med. Chem., 2007, 7, 1817-1828.
    • (2007) Curr. Top. Med. Chem. , vol.7 , pp. 1817-1828
    • Zhang, M.R.1    Suzuki, K.2
  • 382
    • 84978098249 scopus 로고    scopus 로고
    • Schubiger, P.A.; Lehmann, L.; Friebe, M., Eds.; Springer: New York, Ch. 3
    • Wuest, F. In: PET Chemistry - The Driving Force in Molecular Imaging. Schubiger, P.A.; Lehmann, L.; Friebe, M., Eds.; Springer: New York, 2007; Ch. 3 pp. 52-78.
    • (2007) PET Chemistry - The Driving Force in Molecular Imaging , pp. 52-78
    • Wuest, F.1
  • 385
    • 84886250423 scopus 로고    scopus 로고
    • 18F]trifluoromethylation of aryl and heteroaryl iodides for PET imaging
    • 18F]trifluoromethylation of aryl and heteroaryl iodides for PET imaging. Nat. Chem., 2013, 5, 941-944.
    • (2013) Nat. Chem. , vol.5 , pp. 941-944
    • Huiban, M.1    Tredwell, M.2    Mizuta, S.3
  • 386
    • 84904801375 scopus 로고    scopus 로고
    • 18F]trifluoroalkyl groups: Scope and limitations
    • 18F]trifluoroalkyl groups: scope and limitations. BioMed. Res. Int., 2014, 2014, 380124. doi: 10.1155/2014/380124.
    • (2014) BioMed. Res. Int. , vol.2014 , pp. 380124
    • Lien, V.T.1    Riss, P.J.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.