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Structure-activity relationships of alkylamines that inhibit rat liver hydroxysteroid sulfotransferase activities in vitro.

Abstract：

:Tetraalkylammonium salts having n-propyl to n-amyl side chains inhibited rat liver sulfotransferase (ST) activities toward dehydroepiandrosterone and cortisol, but not ST activity toward 2-naphthol, whereas trialkylamines having ethyl to n-amyl side chains inhibited ST activity toward dehydroepiandrosterone, but not ST activities toward cortisol and 2-naphthol. A comparison of I50 values, which represent inhibitor concentration resulting in 50% inhibition of dehydroepiandrosterone ST activity, revealed that the values for the tetraalkylammonium salts were 0.015 to 0.017 mM, whereas the values for the trialkylamines were 0.20 to 0.33 mM. Introduction of hydrophilic groups such as hydroxyl, thiol, nitrile and acetamide groups or substitution by methyl and allyl groups in the alkyl side chains markedly diminished the inhibitory effect of triethylamine. These data indicate that ethyl to n-amyl side chains are a prerequisite for the alkylamine-type inhibitor. Tertiary amine drugs such as imipramine, dimenhydrinate, cyclizine, chlorpromazine and promethazine inhibited ST activities toward dehydroepiandrosterone and cortisol similar to the tetraalkylammonium salts, although the drugs were weaker inhibitors of hydroxysteroid ST activities. These results imply that in addition to trialkylamine side chains, the other portion of the drugs may participate in the inhibition of hydroxysteroid ST activities.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Matsui M,Takahashi M,Miwa Y,Motoyoshi Y,Homma H

doi

10.1016/0006-2952(94)00495-8

subject

Has Abstract

pub_date

1995-03-01 00:00:00

pages

739-41

issue

5

eissn

0006-2952

issn

1873-2968

pii

0006-2952(94)00495-8

journal_volume

49

pub_type

杂志文章

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