Effects of sulfobromophthalein and ethacrynic acid on glyceryl trinitrate relaxation.

Abstract:

:The effects of sulfobromophthalein (SBP) and ethacrynic acid (ECA), both inhibitors of glutathione S-transferase (GST), or glyceryl trinitrate (GTN)-induced vasorelaxation were investigated in rabbit aortic strips. The aortic strips were pre-contracted with phenylephrine, followed by relaxation with 0.5 microM GTN, with or without 0.1 mM SBP or ECA. ECA was observed to inhibit GTN relaxation approximately 32%, whereas SBP did not alter the GTN activity. The dinitrate metabolites (GDN) of GTN in the tissues were also measured. The amounts of both GDNs were decreased in the ECA-treated, but not the SBP-treated group. Moreover, in the ECA-treated group, a strong correlation was obtained between the loss of GTN activity and the decrease in GTN metabolism. Concentration-response studies also revealed that ECA attenuates GTN relaxation. The slope factor of the concentration-response curves was decreased by ECA, but not by SBP, although both inhibitors caused a mild decrease in Emax. In the 9000 g supernatant of rabbit aorta, ECA was also observed to inhibit GTN metabolism more significantly than SBP. The results suggest that the mechanism of GTN activation may involve a GST isozyme that possesses high activities towards ECA.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Lau DT,Benet LZ

doi

10.1016/0006-2952(92)90184-k

subject

Has Abstract

pub_date

1992-05-28 00:00:00

pages

2247-54

issue

10

eissn

0006-2952

issn

1873-2968

pii

0006-2952(92)90184-K

journal_volume

43

pub_type

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