Myocardial accumulation of a dopamine D2 receptor-binding radioligand, 2'-iodospiperone.

Abstract:

:125I-2'-iodospiperone (2'-ISP), which has a high and selective affinity for dopamine D2 receptors, produced a high myocardial accumulation of radioactivity in the early phase after intravenous injection into mice. A human scintigraphic study also showed that the myocardium was clearly visualized soon after intravenous injection of the tracer. Analysis of the myocardial homogenate obtained from mice showed that 125I-2'-ISP was metabolically stable and was taken up the myocardium in its intact form. Administration of spiperone significantly reduced the myocardial uptake of 125I-2'-ISP in mice. Treatment with haloperidol and (+) butaclamol, which have a high affinity for dopamine D2 receptors, also tended to reduce the myocardial uptake of radioactivity, while (-)-butaclamol, which has no affinity for dopamine D2 receptors, caused no change in uptake. These findings suggest that the myocardial accumulation of 2'-ISP occurred in association with dopamine D2 (DA2) receptors.

journal_name

Ann Nucl Med

authors

Saji H,Yonekura Y,Tanahashi K,Iida Y,Iwasaki Y,Magata Y,Konishi J,Yokoyama A

doi

10.1007/BF03164959

subject

Has Abstract

pub_date

1993-08-01 00:00:00

pages

153-6

issue

3

eissn

0914-7187

issn

1864-6433

journal_volume

7

pub_type

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