HOME HELP FEEDBACK SUBSCRIPTIONS ARCHIVE SEARCH TABLE OF CONTENTS		QUICK SEARCH:   [advanced] Author: Keyword(s): Year:  Vol:  Page:

This Article Full Text (PDF) Alert me when this article is cited Alert me if a correction is posted Services Email this article to a friend Similar articles in this journal Similar articles in PubMed Alert me to new issues of the journal Download to citation manager Citing Articles Citing Articles via Google Scholar Google Scholar Articles by Hanson, R. N. Articles by Holmar, B. L. Search for Related Content PubMed PubMed Citation Articles by Hanson, R. N. Articles by Holmar, B. L.

[¹²⁵I]Iodobenzoyl Derivatives of Acebutolol as Potential Myocardial Imaging Agents

Harvard Medical School and Northeastern University, Boston, Massachusetts

Correspondence: For reprints contact: Robert N. Hanson, PhD, Dept. of Medicinal Chemistry and Pharmacology, College of Pharmacy and Allied Health Professions, 360 Huntington Ave., Boston, MA 02115.

ABSTRACT

Three new iodobenzoyl derivatives of acebutolol, a cardioselective beta antagonist, were synthesized and labeled with iodine-125. The biodistributions of these labeled compounds were determined in normal rats and compared with that of thallium-201. Fifteen minutes following i.v. administration, the iodine-125-labeled meta- and para-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 thallium-201 were 2.5 to 3.0 times as high. The data in this study suggest that more lipophilic derivatives of the cardioselective beta antagonists will possess increased uptake and cardioselectivity, and thereby will compare more favorably with thallium-201 as myocardial imaging agents.