PET Imaging of Muscarinic Receptors
Fig. 16.1 Chemical structures of 4-MPB (left), (+)3-MPB and its N-alkyl substitution analogues, (+)3-EPB and (+)3-PPB (right). Affinity (Ki) values of each compound were determined by in vitro assay with…
Current Radioligands for the PET Imaging of Metabotropic Glutamate Receptors
Fig. 15.1 Ionotropic and metabotropic glutamate receptors (Source: http://www.ucl.ac.uk/ioo/research/salt/glutamat.htm (Prof. Tom Salt)) The iGluRs are the principal mediators of excitatory neurotransmission. These are ligand-gated cationic-selective channels which are permeable to…
PET Imaging of Sigma1 Receptors
Fig. 26.1 Chemical structures of clinically used sigma ligands for brain imaging The first radioligand used for imaging sigma1 receptors in the CNS was [11C]SA4503 (Fig. 26.1), which was developed…
PET and SPECT Imaging of Steroid Hormone Receptors
Fig. 14.1 Neurosteroidogenesis: Steroidogenesis follows a sequential, highly compartmentalized reaction, with the translocation of cholesterol from cytoplasm to mitochondria in the cells of CNS, which is mediated by steroidogenic acute…
PET Imaging of ABC Transporters in the BBB
CNS disease ABC transporters examined in the context of this disease References Ischemic stroke ABCB1, ABCC1 ElAli and Hermann (2010), Kilic et al. (2008), Spudich et al. (2006) Epilepsy ABCB1,…
Imaging Type 1 Glycine Transporters in the CNS Using Positron Emission Tomography
Tracer [11C]GSK931145 [18F]MK-6577 [11C]CMPyPB [11C]RO501852 [11C]RO5013853 [11C]-N-Methyl_SSR504734 ([11C]GSK565710) Structure MW 350.51 487.09 499.11 443.19 497.16 410.87 LogD (pH7.4) 2.5 2.9 3.2 2.2 2.3 2.97 pIC50(GlyT1) 8.4 8.7 (human) 8.4…
Principles of Brain Perfusion SPECT
Clinical indication Typical brain perfusion SPECT findings Differential diagnosis in dementia (Borghesani et al. 2010) Alzheimer’s disease (AD) Hypoperfusion of bilateral temporoparietal association cortices (often asymmetric) with characteristic sparing of…
Monoamine Oxidase A and Serotonin Transporter Imaging with Positron Emission Tomography
[11C]Clorgyline [11C]Harmine [11C]Befloxatone Selectivity Excellent (Fowler et al. 1987) Excellent (Bergstrom et al. 1997b) Excellent (Dolle et al. 2003) Reversibility Not reversible (Fowler et al. 1987) Highly reversible (Ginovart…
Cerebral Blood Flow Measurement with Oxygen-15 Water Positron Emission Tomography
Frame duration[s] 5 10 30 Number of frames 24 12 2 The advantageous short half-life of the tracer (122 s) enables the performance of multiple image acquisition scans in rapid…
Cerebral Glucose Metabolism
where C(18F) is the total fluorine activity measured in the tissue, which is determined directly in the PET; C(FDG) is the concentration of free FDG in the tissue, calculated from…
