PET imaging for receptor occupancy: meditations on calculation and simplification

被引:35
|
作者
Zhang, Yumin [1 ]
Fox, Gerard B. [1 ]
机构
[1] Abbott Labs, Global Pharmaceut R&D, Translat Sci, Abbott Pk, IL 60064 USA
来源
JOURNAL OF BIOMEDICAL RESEARCH | 2012年 / 26卷 / 02期
关键词
positron emission tomography; receptor imaging; receptor occupancy; drug development; central nervous system;
D O I
10.1016/S1674-8301(12)60014-1
中图分类号
R-3 [医学研究方法]; R3 [基础医学];
学科分类号
1001 ;
摘要
This invited mini-review briefly summarizes procedures and challenges of measuring receptor occupancy with positron emission tomography. Instead of describing the detailed analytic procedures of in vivo ligand-receptor imaging, the authors provide a pragmatic approach, along with personal perspectives, for conducting positron emission tomography imaging for receptor occupancy, and systematically elucidate the mathematics of receptor occupancy calculations in practical ways that can be understood with elementary algebra. The authors also share insights regarding positron emission tomography imaging for receptor occupancy to facilitate applications for the development of drugs targeting receptors in the central nervous system.
引用
收藏
页码:69 / 76
页数:8
相关论文
共 50 条
  • [41] A pilot PET study of 5-HT1A receptor occupancy by clozapine
    Bantick, RA
    Montgomery, A
    Messa, C
    Grasby, PM
    [J]. SCHIZOPHRENIA RESEARCH, 2000, 41 (01) : 245 - 245
  • [42] An Open Label PET Imaging Study to Evaluate the mGlu5 Receptor Occupancy Following ADX48621 (Dipraglurant) Administration
    Wong, Dean
    Kuwabara, Hiroto
    Poli, Sonia-Maria
    Gapasin, Lorena
    Mathur, Anil
    Carenza, Elisa
    Brasic, James
    George, Noble
    Roberts, Josh
    Kitzmiller, Kelly
    Duvauchelle, Thierry
    [J]. NEUROPSYCHOPHARMACOLOGY, 2017, 42 : S210 - S211
  • [43] Use of Electronic Cigarettes Leads to Significant Beta2-Nicotinic Acetylcholine Receptor Occupancy: Evidence From a PET Imaging Study
    Baldassarri, Stephen R.
    Hillmer, Ansel T.
    Anderson, Jon Mikael
    Jatlow, Peter
    Nabulsi, Nabeel
    Labaree, David
    Cosgrove, Kelly P.
    O'Malley, Stephanie S.
    Eissenberg, Thomas
    Krishnan-Sarin, Suchitra
    Esterlis, Irina
    [J]. NICOTINE & TOBACCO RESEARCH, 2018, 20 (04) : 425 - 433
  • [44] PET imaging of steroid hormone receptor expression
    Allott, Louis
    Smith, Graham
    Aboagye, Eric O.
    Carroll, Laurence
    [J]. Molecular Imaging, 2015, 14 (09) : 534 - 550
  • [45] PET imaging of steroid hormone receptor expression
    Allott, Louis
    Smith, Graham
    Aboagye, Eric O.
    Carroll, Laurence
    [J]. Molecular Imaging, 2015, 14 (10) : 534 - 550
  • [46] PET Imaging of Steroid Hormone Receptor Expression
    Allott, Louis
    Smith, Graham
    Aboagye, Eric O.
    Carroll, Laurence
    [J]. MOLECULAR IMAGING, 2015, 14 : 534 - 550
  • [47] Adenosine Receptor PET Imaging in Human Brain
    Mishina, Masahiro
    Ishiwata, Kiich
    [J]. ADENOSINE RECEPTORS IN NEUROLOGY AND PSYCHIATRY, 2014, 119 : 51 - 69
  • [48] PET Imaging of Receptor Tyrosine Kinases in Cancer
    Wei, Weijun
    Ni, Dalong
    Ehlerding, Emily B.
    Luo, Quan-Yong
    Cai, Weibo
    [J]. MOLECULAR CANCER THERAPEUTICS, 2018, 17 (08) : 1625 - 1636
  • [49] PET oestrogen receptor imaging: ready for the clinic?
    Mankoff, David A.
    Clark, Amy S.
    [J]. LANCET ONCOLOGY, 2019, 20 (04): : 467 - 469
  • [50] Quantitative PET Imaging of VEGF Receptor Expression
    Kai Chen
    Weibo Cai
    Zi-Bo Li
    Hui Wang
    Xiaoyuan Chen
    [J]. Molecular Imaging and Biology, 2009, 11 : 15 - 22