Synthesis and evaluation of radiolabeled antagonists for imaging of β-adrenoceptors in the brain with PET

被引：25

作者：

Doze, P ^{[1
]}

Elsinga, PH ^{[1
]}

Maas, B ^{[1
]}

Van Waarde, A ^{[1
]}

Wegman, T ^{[1
]}

Vaalburg, W ^{[1
]}

机构：

[1] Univ Groningen Hosp, PET Ctr, NL-9700 RB Groningen, Netherlands

来源：

NEUROCHEMISTRY INTERNATIONAL | 2002年 / 40卷 / 02期

关键词：

PET; beta-adrenoceptors; brain;

D O I：

10.1016/S0197-0186(01)00081-X

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

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, [I-125]-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. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：145 / 155

页数：11

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