Myocardial and pulmonary uptake of S-1'-[18F]fluorocarazolol in intact rats reflects radioligand binding to beta-adrenoceptors

European Journal of Pharmacology
A Van WaardeW Vaalburg

Abstract

The biodistribution of S-(-)-4-(2-hydroxy-3-(1'-[18F]fluoroisopropyl)- aminopropoxy)carbazole ([18F]S-fluorocarazolol, a non-selective beta-adrenoceptor antagonist) was studied in rats (60 min after 18F injection when specific binding in peripheral organs was maximal). 18F uptake in brain, erythrocytes, heart and lung appeared to be linked to beta-adrenoceptors. CGP-20712A and ICI-89,406 inhibited 18F uptake in heart (predominantly beta 1-adrenoceptors) more potently than in lungs (predominantly beta 2-adrenoceptors). In contrast, ICI-118,551 and procaterol were more potent in the lungs than in the heart. ICI-118,551 inhibited 18F uptake in cerebellum (predominantly beta 2-adrenoceptors) more potently than in cerebral cortex (predominantly beta 1-adrenoceptors). Stereoselectivity of the in vivo binding was demonstrated since S-(-)-propranolol inhibited uptake in target tissues more effectively than R-(+)-propranolol. Myocardial and cerebral imaging may be hampered by poor heart-to-lung contrast and low signal-to-noise ratios, but [18F]S-fluorocarazolol seems suitable for positron emission tomography (PET) of pulmonary beta-adrenoceptors.

References

Jul 20, 1979·Naunyn-Schmiedeberg's Archives of Pharmacology·S R NahorskiE L Rugg
Dec 1, 1979·Thorax·D M GeddesJ P Blackburn
May 1, 1976·British Journal of Pharmacology·C T Dollery, A F Junod
Oct 1, 1992·International Journal of Radiation Applications and Instrumentation. Part B, Nuclear Medicine and Biology·A Van WaardeK I Lie
Jul 1, 1992·Naunyn-Schmiedeberg's Archives of Pharmacology·L J Bryan-Lluka, S R O'Donnell
Sep 1, 1991·Journal of Neurochemistry·B H Erdtsieck-ErnsteG J Boer
Oct 17, 1989·European Journal of Pharmacology·P VanscheeuwijckN Fraeyman
Sep 1, 1985·Naunyn-Schmiedeberg's Archives of Pharmacology·E N JubergP W Abel
Oct 14, 1986·European Journal of Pharmacology·D J DooleyN C Reymann
Mar 17, 1986·FEBS Letters·K KramerA Bast
May 1, 1987·Proceedings of the Society for Experimental Biology and Medicine·C A Schneyer, M G Humphreys-Beher
Oct 22, 1981·European Journal of Pharmacology·E A Stone, D C U'Prichard
Sep 1, 1983·The Journal of Pharmacy and Pharmacology·B CostinJ C Wanstall
May 1, 1983·Journal of Cardiovascular Pharmacology·A J BilskiJ L Wale
Aug 27, 1981·European Journal of Pharmacology·K E Dickinson, S R Nahorski
Jan 1, 1981·Journal of Neuroscience Research·K KuriyamaZ P Ping
Sep 30, 1983·European Journal of Pharmacology·D Bojanic, S R Nahorski
Mar 1, 1984·Proceedings of the National Academy of Sciences of the United States of America·T C RainbowB B Wolfe
May 1, 1981·British Journal of Pharmacology·B A Hemsworth, J A Street

Citations

Feb 26, 2010·Journal of Nuclear Cardiology : Official Publication of the American Society of Nuclear Cardiology·Miran KenkRob S Beanlands
Oct 9, 2004·Journal of Nuclear Cardiology : Official Publication of the American Society of Nuclear Cardiology·Frank M Bengel, Markus Schwaiger
May 17, 2000·Pharmaceutica acta Helvetiae·V W PikeP G Camici
Nov 28, 2002·Nuclear Medicine and Biology·H ValetteDaniel Marzin
Oct 1, 2003·Clinical Positron Imaging : Official Journal of the Institute for Clinical P.E.T·P H ElsingaWillem Vaalburg
Sep 1, 2005·European Journal of Nuclear Medicine and Molecular Imaging·Andreas HelischPeter Bartenstein

Related Concepts

4-(3-tert-butylamino-2-hydroxypropoxy)benzimidazol-2-one, 2-(11)C-labeled
Fluorocarazolol, (R-(R*, R*))-stereoisomer
Adrenergic beta-Antagonists
Metazoa
Carbazoles
Thorazine
Fluorine Radioisotopes
Novodrin
Lung
Myocardium

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.