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Effects of the new ethacrynic acid derivative SA9000 on intraocular pressure in cats and monkeys.

Publication ,  Journal Article
Shimazaki, A; Ichikawa, M; Rao, PV; Kirihara, T; Konomi, K; Epstein, DL; Hara, H
Published in: Biol Pharm Bull
July 2004

To evaluate the pharmacological characteristics of the new ethacrynic acid (ECA) derivative SA9000, we examined its ocular hypotensive effects in cats and cynomolgus monkeys, its corneal toxicity in rabbits, and its binding affinities for forty-three receptors, ion channels, and second messenger systems. A 20 microl injection into the anterior chamber of eye (intracameral injection) of 0.1 mM SA9000 significantly reduced intraocular pressure (IOP) 3.8 mmHg in cats. A 10 microl intracameral injection of 1 mM SA9000 significantly reduced IOP 7 mmHg in living monkeys without evidence of in vivo (or in vitro) toxicity. The ocular hypotensive effect of SA9000 in monkeys was greater than that of ECA. The morphology of corneal endothelial and epithelial cells in rabbit eyes after intracameral injection of SA9000 was observed using electron microphotography. SA9000 at 2 mM did not induce any abnormalities, indicating that it has no corneal toxicity at a concentration higher than the minimum needed for an ocular hypotensive effect (1 mM). SA9000 at 0.01 mM showed negligible binding affinity for, or inhibition of, forty-three different receptors, ion channel proteins, and second messenger systems. These findings indicate that SA9000 has the potential to be both effective and safe as an ocular hypotensive drug, although the mechanism of action remains unclear.

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Published In

Biol Pharm Bull

DOI

ISSN

0918-6158

Publication Date

July 2004

Volume

27

Issue

7

Start / End Page

1019 / 1024

Location

Japan

Related Subject Headings

  • Rabbits
  • Pharmacology & Pharmacy
  • Macaca fascicularis
  • Intraocular Pressure
  • Ethacrynic Acid
  • Dose-Response Relationship, Drug
  • Diuretics
  • Cornea
  • Cinnamates
  • Cats
 

Citation

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Shimazaki, A., Ichikawa, M., Rao, P. V., Kirihara, T., Konomi, K., Epstein, D. L., & Hara, H. (2004). Effects of the new ethacrynic acid derivative SA9000 on intraocular pressure in cats and monkeys. Biol Pharm Bull, 27(7), 1019–1024. https://doi.org/10.1248/bpb.27.1019
Shimazaki, Atsushi, Masaki Ichikawa, Ponugoti Vasantha Rao, Tomoko Kirihara, Kouji Konomi, David Lee Epstein, and Hideaki Hara. “Effects of the new ethacrynic acid derivative SA9000 on intraocular pressure in cats and monkeys.Biol Pharm Bull 27, no. 7 (July 2004): 1019–24. https://doi.org/10.1248/bpb.27.1019.
Shimazaki A, Ichikawa M, Rao PV, Kirihara T, Konomi K, Epstein DL, et al. Effects of the new ethacrynic acid derivative SA9000 on intraocular pressure in cats and monkeys. Biol Pharm Bull. 2004 Jul;27(7):1019–24.
Shimazaki, Atsushi, et al. “Effects of the new ethacrynic acid derivative SA9000 on intraocular pressure in cats and monkeys.Biol Pharm Bull, vol. 27, no. 7, July 2004, pp. 1019–24. Pubmed, doi:10.1248/bpb.27.1019.
Shimazaki A, Ichikawa M, Rao PV, Kirihara T, Konomi K, Epstein DL, Hara H. Effects of the new ethacrynic acid derivative SA9000 on intraocular pressure in cats and monkeys. Biol Pharm Bull. 2004 Jul;27(7):1019–1024.

Published In

Biol Pharm Bull

DOI

ISSN

0918-6158

Publication Date

July 2004

Volume

27

Issue

7

Start / End Page

1019 / 1024

Location

Japan

Related Subject Headings

  • Rabbits
  • Pharmacology & Pharmacy
  • Macaca fascicularis
  • Intraocular Pressure
  • Ethacrynic Acid
  • Dose-Response Relationship, Drug
  • Diuretics
  • Cornea
  • Cinnamates
  • Cats