[IODOBENZOYL-I-125 DERIVATIVES OF ACEBUTOLOL AS POTENTIAL MYOCARDIAL IMAGING AGENTS

  • 1 January 1980
    • journal article
    • research article
    • Vol. 21 (9), 846-851
Abstract
Three new iodobenzoyl derivatives of acebutolol, a cardioselective .beta.-antagonist, were synthesized and labeled with 125I. The biodistributions of these labeled compounds were determined in normal rats and compared with that of 201Tl. Fifteen minutes following i.v. administration, the 125I-labeled m- to p-iodobenzoyl acebutolols possessed the greatest ventricular uptake and the highest ventricle-to-blood and ventricle-to-lung ratios of the new agents. The corresponding values for 201Tl were 2.5-3.0 times as high. More lipophilic derivatives of the cardioselective .beta.-antagonists will possess increased uptake and cardioselectivity, and thereby will compare more favorably with 201Tl as myocardial imaging agents.