Synthesis and evaluation of radiolabeled antagonists for imaging of beta-adrenoceptors in the brain with PET.
Petra Doze, P H Elsinga, B Maas, A Van Waarde, T Wegman, W Vaalburg
Index: Neurochem. Int. 40(2) , 145-55, (2002)
Full Text: HTML
Abstract
Five potent, lipophilic beta-adrenoceptor antagonists (carvedilol, pindolol, toliprolol and fluorinated analogs of bupranolol and penbutolol) were labeled with either carbon-11 or fluorine-18 and evaluated for cerebral beta-adrenoceptor imaging in experimental animals. The standard radioligand for autoradiography of beta-adrenoceptors, [125I]-iodocyanopindolol, was also included in this survey. All compounds showed either very low uptake in rat brain or a regional distribution that was not related to beta-adrenoceptors, whereas some ligands did display specific binding in heart and lungs. Apparently, the criteria of a high affinity and a moderately high lipophilicity were insufficient to predict the suitability of beta-adrenergic antagonists for visualization of beta-adrenoceptors in the central nervous system.
Related Compounds
Related Articles:
Regioselective alkylation of phenol with cyclopentanol over montmorillonite K10: An efficient synthesis of 1-(2-cyclopentylphenoxy)-3-[(1, 1-dimethylethyl) amino] propan-2-ol {(S)-penbutolol}. Phukan P and Sudalai A.
[J. Chem. Soc. Perkin Trans. I 20 , 3015-18, (1999)]