Effects of 2-Nicotinamidethyl Nitrate (SG-75), a New Antianginal Drug, on the Cyclic AMP Phosphodiesterase Activity

Masao Endoh; Teruyuki Yanagisawa; Norio Taira

doi:10.1620/tjem.130.199

Effects of 2-Nicotinamidethyl Nitrate (SG-75), a New Antianginal Drug, on the Cyclic AMP Phosphodiesterase Activity

Masao Endoh, Teruyuki Yanagisawa, Norio Taira

MED - Medical Sciences

Research output: Contribution to journal › Article › peer-review

16 Citations (Scopus)

Abstract

The effect of a potent coronary vasodilator, SG-75, on the purified cyclic AMP phosphodiesterase of the bovine heart was compared with that of papaverine. SG-75 inhibited the phosphodiesterase activity in a competitive manner, the IC₅₀ being 10 mM. SG-75 was approximately 300 times less potent than papaverine in inhibiting the phosphodiesterase activity. Thus, it is unlikely that the phosphodiesterase inhibition by SG-75 is involved in its vasodilator action.

Original language	English
Pages (from-to)	199-201
Number of pages	3
Journal	the tohoku journal of experimental medicine
Volume	130
Issue number	2
DOIs	https://doi.org/10.1620/tjem.130.199
Publication status	Published - 1980

Keywords

2-nicotinamidethyl nitrate
antianginal drug
coronary vasodilator
cyclic AMP phosphodiesterase
papaverine

ASJC Scopus subject areas

Biochemistry, Genetics and Molecular Biology(all)

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title = "Effects of 2-Nicotinamidethyl Nitrate (SG-75), a New Antianginal Drug, on the Cyclic AMP Phosphodiesterase Activity",

abstract = "The effect of a potent coronary vasodilator, SG-75, on the purified cyclic AMP phosphodiesterase of the bovine heart was compared with that of papaverine. SG-75 inhibited the phosphodiesterase activity in a competitive manner, the IC50 being 10 mM. SG-75 was approximately 300 times less potent than papaverine in inhibiting the phosphodiesterase activity. Thus, it is unlikely that the phosphodiesterase inhibition by SG-75 is involved in its vasodilator action.",

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AU - Taira, Norio

PY - 1980

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N2 - The effect of a potent coronary vasodilator, SG-75, on the purified cyclic AMP phosphodiesterase of the bovine heart was compared with that of papaverine. SG-75 inhibited the phosphodiesterase activity in a competitive manner, the IC50 being 10 mM. SG-75 was approximately 300 times less potent than papaverine in inhibiting the phosphodiesterase activity. Thus, it is unlikely that the phosphodiesterase inhibition by SG-75 is involved in its vasodilator action.

AB - The effect of a potent coronary vasodilator, SG-75, on the purified cyclic AMP phosphodiesterase of the bovine heart was compared with that of papaverine. SG-75 inhibited the phosphodiesterase activity in a competitive manner, the IC50 being 10 mM. SG-75 was approximately 300 times less potent than papaverine in inhibiting the phosphodiesterase activity. Thus, it is unlikely that the phosphodiesterase inhibition by SG-75 is involved in its vasodilator action.

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KW - cyclic AMP phosphodiesterase

KW - papaverine

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