Validation of S-1'-[18F]fluorocarazolol for in vivo imaging and quantification of cerebral beta-adrenoceptors

European Journal of Pharmacology
P DozeW Vaalburg

Abstract

S-1'-[18F]fluorocarazolol (S-(-)-4-(2-hydroxy-3-(1'-[18F]fluoroisopropyl)-aminopropoxy)carba zole, a non-subtype-selective beta-adrenoceptor antagonist) has been investigated for in vivo studies of beta-adrenoceptors. Previous results indicated that uptake of this radioligand in heart and lung can be inhibited by beta-adrenoceptor agonists and antagonists. In the present study, blocking, displacement and saturation experiments were performed in rats, in combination with metabolite analysis to investigate the suitability of this radioligand for in vivo positron emission tomography (PET) imaging and quantification of beta-adrenoceptors in the brain. The results demonstrate that, (i) the uptake of S-1'-[18F]fluorocarazolol reflects specific binding to beta-adrenoceptors, (ii) binding of S-1'-[18F]fluorocarazolol to atypical or non-beta-adrenergic sites is negligible, (iii) uptake of radioactive metabolites in the brain is less than 25% of total radioactivity, 60 min after injection, (iv) in vivo measurements of receptor densities (Bmax) in cortex, cerebellum, heart, lung and erythrocytes are within range of densities determined from in vitro assays, (v) binding of S-1'-[18F]fluorocarazolol can be displaced. In conclusion, S-1'-[18...Continue Reading

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Citations

Apr 7, 2009·Journal of Pharmacological Sciences·Terumasa HashimotoKazuo Honda
Sep 10, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Santosh Reddy AlluriKun-Eek Kil
May 25, 2005·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Philip H ElsingaWillem Vaalburg
Nov 3, 2004·CNS Spectrums·J McConathyM M Goodman

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