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KMID : 0043319910140040290
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Archives of Pharmacal Research
1991 Volume.14 No. 4 p.290 ~ p.294
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Determination of Peripheral Catechol O-methyltransferase (COMT) Activity in vivo using [2-14C]-3’’,4’’-Dihydroxyacetophenone
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Kim EJ
Ahn JW/Lee HS/Christ W
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Abstract
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For the determination of peripheral COMT activity, we synthesized [2-14C]-3’’,4’’-dihydroxyacetophenone([14C]-DHAP), a model substrate closely related to catecholamines, which cannot be attacked by monoamine oxidase. After iv.-injection of [14C]-DHAP in living animals, only 3’’,4’’-dihydroxy-acetophenone (3’’,4’’-DHAP) and 3’’-methoxy-4’’-hydroxyacetophenone (3’’-MHAP) were detected in blood by thin layer radio chromatography. It could be speculated that 3’’,4’’-DHAP was primarily 0-methylated by COMT, followed by subsequent conjugations. The concentration of 3’’,4’’-DHAP, a substrate for COMT, in blood at 5min after injection of [14C]-DHAP, were similar in all animals. The rate of 3’’-MHAP formation can be therefore used as an indicator for peripheral COMT activity. The velocity of methylation in 15min after i.v.-administration of [14C]-DHAP was 0.28mcg/ml.min. From these results, 3’’,4’’-DHAP was shown to be used as an appropriate substrate to determine the COMT activity in vivo.
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