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

European Journal of Pharmacology
P DozeW Vaalburg


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


Jul 1, 1979·Journal of Neurochemistry·J W SchweitzerA J Friedhoff
Jan 1, 1992·The American Journal of Clinical Nutrition·L J EmorineD A Strosberg
Jan 1, 1992·Pharmacology & Toxicology·F De PaermentierR W Horton
Jan 1, 1990·British Journal of Pharmacology·N TumerJ Roberts
Dec 1, 1989·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·S C HuangM E Phelps
Sep 1, 1989·Experimental Neurology·P ValveriusB Tabakoff
Sep 8, 1989·Science·L J EmorineA D Strosberg
Nov 1, 1985·Proceedings of the National Academy of Sciences of the United States of America·J B FlexnerD J Brunswick
Apr 29, 1986·European Journal of Pharmacology·A Biegon, M Israeli
Mar 1, 1987·Journal of Autonomic Pharmacology·M C MichelO E Brodde
Dec 16, 1973·Life Sciences·O M BakkeC T Dollery
Apr 15, 1982·Brain Research·E A Stone, J E Platt
Mar 1, 1984·Proceedings of the National Academy of Sciences of the United States of America·T C RainbowB B Wolfe
Jun 1, 1995·Pharmacology, Biochemistry, and Behavior·E A StoneD Quartermain
Jun 1, 1995·Pharmacology, Biochemistry, and Behavior·S K BrannanF Petty
Apr 1, 1993·Experimental Neurology·J Sutin, R Griffith
Apr 12, 1996·Journal of Chromatography. B, Biomedical Applications·A van WaardeW Vaalburg

❮ Previous
Next ❯


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

❮ Previous
Next ❯

Related Concepts

Related Feeds

Adrenergic Receptors: Trafficking

Adrenergic receptor trafficking is an active physiological process where adrenergic receptors are relocated from one region of the cell to another or from one type of cell to another. Discover the latest research on adrenergic receptor trafficking here.