A business of some heat: molecular imaging of phosphodiesterase 5

Cumming, Paul (2016) A business of some heat: molecular imaging of phosphodiesterase 5. Journal of Neurochemistry, 136(2), pp. 220-221.

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Abstract

G-protein coupled receptors activate intracellular signaling by well-known pathways involving cyclic nucleotides or phosphatidylinositol. However, these signaling pathways (second messenger systems) have scarcely been investigated with molecular imaging techniques. This Editorial highlights a preclinical PET study by Gómez-Vallejo and coworkers, in which the authors studied the cerebral uptake of the prototypic phosphodiesterase 5 (PDE5) inhibitor sildenafil and showed that its action manifested in elevated cGMP levels in cerebrospinal fluid of non-human primates, but their rat PET studies with [11C]sildenafil failed to show specific binding in brain. This negative PET study underlines that abundance (Bmax) of the target molecule can be decisive for success of a new ligand, and emphasizes the need for further quantitative PET studies of PDE5 as calculations suggest that it might yet be detected with a PET tracer of higher affinity than [11C]sildenafil.

Impact and interest:

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ID Code: 99692
Item Type: Journal Article
Refereed: Yes
DOI: 10.1111/jnc.13453
ISSN: 1471-4159
Subjects: Australian and New Zealand Standard Research Classification > PSYCHOLOGY AND COGNITIVE SCIENCES (170000) > PSYCHOLOGY (170100) > Biological Psychology (Neuropsychology Psychopharmacology Physiological Psychology) (170101)
Divisions: Current > QUT Faculties and Divisions > Faculty of Health
Current > Institutes > Institute of Health and Biomedical Innovation
Current > Schools > School of Psychology & Counselling
Copyright Owner: 2016 International Society for Neurochemistry
Deposited On: 13 Oct 2016 00:24
Last Modified: 13 Oct 2016 21:25

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