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New ethacrynic acid derivatives as potent cytoskeletal modulators in trabecular meshwork cells.

Publication ,  Journal Article
Shimazaki, A; Suhara, H; Ichikawa, M; Matsugi, T; Konomi, K; Takagi, Y; Hara, H; Rao, PV; Epstein, DL
Published in: Biol Pharm Bull
June 2004

A series of ethacrynic acid (ECA) derivatives were synthesized and examined for ocular hypotensive activity. Efficacy was evaluated in a cell-shape assay, using human trabecular meshwork cells, and cytotoxicity in a (3-(4,5-dimethylthiazole-2-yl)-5-(3-carboxymethoxy phenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay, using cultured bovine trabecular meshwork cells. Many of the derivatives demonstrated efficacy equal to or greater than that of ECA. SA9000 was selected as the most promising candidate for a novel ocular hypotensive drug with few side effects.

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Published In

Biol Pharm Bull

DOI

ISSN

0918-6158

Publication Date

June 2004

Volume

27

Issue

6

Start / End Page

846 / 850

Location

Japan

Related Subject Headings

  • Trabecular Meshwork
  • Pharmacology & Pharmacy
  • Ethacrynic Acid
  • Cytoskeleton
  • Cells, Cultured
  • Cattle
  • Animals
  • 3404 Medicinal and biomolecular chemistry
  • 3214 Pharmacology and pharmaceutical sciences
  • 3101 Biochemistry and cell biology
 

Citation

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Shimazaki, A., Suhara, H., Ichikawa, M., Matsugi, T., Konomi, K., Takagi, Y., … Epstein, D. L. (2004). New ethacrynic acid derivatives as potent cytoskeletal modulators in trabecular meshwork cells. Biol Pharm Bull, 27(6), 846–850. https://doi.org/10.1248/bpb.27.846
Shimazaki, Atsushi, Hiroshi Suhara, Masaki Ichikawa, Takeshi Matsugi, Koji Konomi, Yasutaka Takagi, Hideaki Hara, Ponugoti Vasantha Rao, and David Lee Epstein. “New ethacrynic acid derivatives as potent cytoskeletal modulators in trabecular meshwork cells.Biol Pharm Bull 27, no. 6 (June 2004): 846–50. https://doi.org/10.1248/bpb.27.846.
Shimazaki A, Suhara H, Ichikawa M, Matsugi T, Konomi K, Takagi Y, et al. New ethacrynic acid derivatives as potent cytoskeletal modulators in trabecular meshwork cells. Biol Pharm Bull. 2004 Jun;27(6):846–50.
Shimazaki, Atsushi, et al. “New ethacrynic acid derivatives as potent cytoskeletal modulators in trabecular meshwork cells.Biol Pharm Bull, vol. 27, no. 6, June 2004, pp. 846–50. Pubmed, doi:10.1248/bpb.27.846.
Shimazaki A, Suhara H, Ichikawa M, Matsugi T, Konomi K, Takagi Y, Hara H, Rao PV, Epstein DL. New ethacrynic acid derivatives as potent cytoskeletal modulators in trabecular meshwork cells. Biol Pharm Bull. 2004 Jun;27(6):846–850.

Published In

Biol Pharm Bull

DOI

ISSN

0918-6158

Publication Date

June 2004

Volume

27

Issue

6

Start / End Page

846 / 850

Location

Japan

Related Subject Headings

  • Trabecular Meshwork
  • Pharmacology & Pharmacy
  • Ethacrynic Acid
  • Cytoskeleton
  • Cells, Cultured
  • Cattle
  • Animals
  • 3404 Medicinal and biomolecular chemistry
  • 3214 Pharmacology and pharmaceutical sciences
  • 3101 Biochemistry and cell biology