Synthesis and evaluation of [123I]-iodo-PK11195 for mapping peripheral-type benzodiazepine receptors (omega 3) in heart.

Abstract:

:An iodinated analog of PK11195, 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)isoquinoline-3-carboxamide , a specific antagonist of the peripheral-type benzodiazepine receptor (omega 3), has been synthesized in three steps with an overall chemical yield of 40%. Both [123I]- and [125I]-Iodo-PK11195 have been synthesized by solid-state isotopic exchange in > 60% isolated radiochemical yield and specific activity of 233-348 mCi/mmol. Tissue distribution studies in rats indicate a high uptake of radioactivity in adrenal glands, heart, lung and kidneys, which was blocked 63-87% by preadministration of cold PK11195. Single photon emission computer tomography (SPECT) imaging of the canine heart has been accomplished with [123I]PK11195. These results suggest that [123I]PK11195 has potential as a SPECT radiotracer for studying the omega 3 receptor in humans.

journal_name

Nucl Med Biol

authors

Gildersleeve DL,Van Dort ME,Johnson JW,Sherman PS,Wieland DM

doi

10.1016/0969-8051(95)02007-1

subject

Has Abstract

pub_date

1996-01-01 00:00:00

pages

23-8

issue

1

eissn

0969-8051

issn

1872-9614

pii

0969-8051(95)02007-1

journal_volume

23

pub_type

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