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

PET-Center, Groningen University Hospital, P.O. Box 30.001, 9700 RB Groningen, The Netherlands.

Neurochemistry international 2002 Feb

filter terms:

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.

Citation

Petra Doze, P H Elsinga, B Maas, A Van Waarde, T Wegman, W Vaalburg. Synthesis and evaluation of radiolabeled antagonists for imaging of beta-adrenoceptors in the brain with PET. Neurochemistry international. 2002 Feb;40(2):145-55