157989-11-2Relevant articles and documents
Myocardial and pulmonary uptake of S-1'-[18F]fluorocarazolol in intact rats reflects radioligand binding to β-adrenoceptors
Van Waarde,Elsinga,Brodde,Visser,Vaalburg
, p. 159 - 168 (1995)
The biodistribution of S-(-)-4-(2-hydroxy-3-(1'-[18F]fluoroisopropyl)- aminopropoxy)carbazole ([18F]S-fluorocarazolol, a non-selective β-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 β-adrenoceptors. CGP-20712A and ICI-89,406 inhibited 18F uptake in heart (predominantly, β1-adrenoceptors) more potently than in lungs (predominantly β2-adrenoceptors). In contrast, ICI-118,551 and procaterol were more potent in the lungs than in the heart. ICI-118,551 inhibited F uptake in cerebellum (predominantly, β2-adrenoceptors) more potently than in cerebral cortex (predominantly, β1-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, β-adrenoceptors.
Synthesis, binding properties, and 18F labeling of fluorocarazolol, a high-affinity β-adrenergic receptor antagonist
Zheng,Berridge,Ernsberger
, p. 3219 - 3230 (1994)
New β-adrenergic receptor antagonists, 2-(R)-(+)- and 2-(S)-(-)-1-(9H- carbazol-4-yl-oxy)-3-[[1-(fluoromethyl)ethyl]amino]-2-propanol ((S)- and (R)- fluorocarazolols), were labeled with fluorine-18 at the no-carrier-added level by reductive alkylation of
