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首页> 外文期刊>Neurochemistry International: The International Journal for the Rapid Publication of Critical Reviews, Preliminary and Original Research Communications in Neurochemistry >Synthesis and evaluation of radiolabeled antagonists for imaging of beta-adrenoceptors in the brain with PET.
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Synthesis and evaluation of radiolabeled antagonists for imaging of beta-adrenoceptors in the brain with PET.

机译：PET合成和评估用于脑中β-肾上腺素能受体成像的放射性标记拮抗剂。

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摘要

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.
机译：用碳11或氟18标记五种有效的亲脂性β-肾上腺素受体拮抗剂（卡维地洛，品多洛尔，托普洛尔和丁苯洛尔和戊丁醇的氟化类似物），并在实验动物中评估其脑β-肾上腺素受体成像。 β-肾上腺素受体放射自显影的标准放射性配体[125I]-碘氰基吲哚洛尔也包括在这项调查中。所有化合物在大鼠脑中的摄取都很低，或与β-肾上腺素受体无关的区域分布，而某些配体确实在心脏和肺部表现出特异性结合。显然，高亲和力和中等亲脂性的标准不足以预测β-肾上腺素能拮抗剂在中枢神经系统中可视化β-肾上腺素能受体的适用性。

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