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Chemical Compound Review:

AG-K-52576 N-(3,4-dioxo-1-phenyl-7- pyridin-2-yloxy...

Synonyms: LS-9646, NK-3201, AC1Q5BUH, CTK1A5741, DCL000786, ...

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Disease relevance of NK-3201

A novel chymase inhibitor, 2-(5-formylamino-6-oxo-2-phenyl-1,6-dihydropyrimidine-1-yl)-N-[[,4-dioxo-1-phenyl-7-(2-pyridyloxy)]2-heptyl]acetamide (NK3201), suppressed intimal hyperplasia after balloon injury [1].
A specific chymase inhibitor, 2-(5-formylamino-6-oxo-2-phenyl-1,6-dihydropyrimidine-1-yl)-N-[[3,4-dioxo-1-phenyl-7-(2-pyridyloxy)]-2-heptyl]acetamide (NK3201), suppresses development of abdominal aortic aneurysm in hamsters [2].
Therefore, NK3201 may be useful in the prevention of pulmonary fibrosis [3].
One day after the ligation, rats were randomized into 2 groups: 1) a chymase-treated group that received 10 mg/kg per day of the chymase inhibitor NK3201 orally for 4 weeks; and 2) a vehicle group of non-treated rats with myocardial infarction [4].

High impact information on NK-3201

Four weeks after balloon injury, NK3201 did not affect the plasma renin and angiotensin-converting enzyme activities [1].
A specific chymase inhibitor, NK3201, suppresses bleomycin-induced pulmonary fibrosis in hamsters [3].
We evaluated whether a chymase inhibitor, 2-(5-formylamino-6-oxo-2-phenyl-1,6-dihydropyrimidine-1-yl)-N-[(3,4-dioxo-1-phenyl-7-(2-pyridyloxy))-2-heptyl]acetamide (NK3201), suppressed bleomycin-induced pulmonary fibrosis [3].
A significant increase of chymase activity in the injured uterus was reduced by treatment with NK3201 [5].
Recently, however, the chymase inhibitor NK3201 (2-(5-formylamino-6-oxo-2-phenyl-1,6-dihydropyrimidin-1-yl)-N-[[3,4-dioxo-1-phenyl-7-(2-pyridyloxy)]-2-heptyl] acetamide) was demonstrated to have oral activity against neointimal hyperplasia in dog models (Takai S. et al., Life Sci 69, 1725 - 1732 (2001)) [6].

Biological context of NK-3201

Therefore, NK3201 may be useful for preventing vascular proliferation without affecting blood pressure [7].

Anatomical context of NK-3201

In this study, we investigated whether an orally active chymase inhibitor, 2-(5-formylamino-6-oxo-2-phenyl-1,6-dihydropyrimidine-1-yl)-N-[[3,4-dioxo-1-phenyl-7-(2-pyridyloxy)]-2-heptyl]acetamide (NK3201), prevents intimal hyperplasia in carotid arteries injured by a balloon catheter in dog [1].

Associations of NK-3201 with other chemical compounds

Hamsters were orally administered NK3201 (30 mg/kg per day) or placebo, beginning 5 days before intratracheal instillation of bleomycin (10 mg/kg) [3].
On the other hand, NK3201, unlike angiotensin converting enzyme inhibitors or angiotensin II receptor blockers, did not affect blood pressure [7].
On the other hand, NK3201 does not inhibit other types of serine proteases, tryptase, thrombin, elastase, plasmin, and plasminogen activator [7].

Analytical, diagnostic and therapeutic context of NK-3201

Oral administration of NK3201 may be a useful drug for prevention of peritoneal adhesion formation [5].

References

A novel chymase inhibitor, 2-(5-formylamino-6-oxo-2-phenyl-1,6-dihydropyrimidine-1-yl)-N-[[,4-dioxo-1-phenyl-7-(2-pyridyloxy)]2-heptyl]acetamide (NK3201), suppressed intimal hyperplasia after balloon injury. Takai, S., Sakonjo, H., Fukuda, K., Jin, D., Sakaguchi, M., Kamoshita, K., Ishida, K., Sukenaga, Y., Miyazaki, M. J. Pharmacol. Exp. Ther. (2003) [Pubmed]
A specific chymase inhibitor, 2-(5-formylamino-6-oxo-2-phenyl-1,6-dihydropyrimidine-1-yl)-N-[[3,4-dioxo-1-phenyl-7-(2-pyridyloxy)]-2-heptyl]acetamide (NK3201), suppresses development of abdominal aortic aneurysm in hamsters. Tsunemi, K., Takai, S., Nishimoto, M., Jin, D., Sakaguchi, M., Muramatsu, M., Yuda, A., Sasaki, S., Miyazaki, M. J. Pharmacol. Exp. Ther. (2004) [Pubmed]
A specific chymase inhibitor, NK3201, suppresses bleomycin-induced pulmonary fibrosis in hamsters. Sakaguchi, M., Takai, S., Jin, D., Okamoto, Y., Muramatsu, M., Kim, S., Miyazaki, M. Eur. J. Pharmacol. (2004) [Pubmed]
Chymase inhibition prevents cardiac fibrosis and dysfunction after myocardial infarction in rats. Kanemitsu, H., Takai, S., Tsuneyoshi, H., Nishina, T., Yoshikawa, K., Miyazaki, M., Ikeda, T., Komeda, M. Hypertens. Res. (2006) [Pubmed]
Oral administration of a novel chymase inhibitor, NK3201, prevents peritoneal adhesion formation in hamsters. Okamoto, Y., Takai, S., Miyazaki, M. Jpn. J. Pharmacol. (2002) [Pubmed]
Development of the chymase inhibitor as an anti-tissue-remodeling drug: myocardial infarction and some other possibilities. Sukenaga, Y., Kamoshita, K., Takai, S., Miyazaki, M. Jpn. J. Pharmacol. (2002) [Pubmed]
Application of a chymase inhibitor, NK3201, for prevention of vascular proliferation. Takai, S., Miyazaki, M. Cardiovascular drug reviews. (2003) [Pubmed]

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