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Chemical Compound Review

LS-55815     (4R)-4-[[(2R)-2-[[(2S)-2- [[(2R,3S)-2...

Synonyms: BE-18257B, AC1L538E, BE 18257B, 136553-74-7
 
 
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Disease relevance of BE-18257B

  • METHODS AND RESULTS: We measured plasma ET-1 concentrations by radioimmunoassay in isolated blood-perfused neonatal lamb hearts before and after 2 hours of 10 degrees C cardioplegic ischemia and examined the effects of ET-1 and the endothelin-A (ET-A) receptor antagonist BE-18257B on the postischemic recovery of isolated hearts [1].
  • A competitive endothelin (ET) antagonist, BE-18257B, was isolated from the fermentation products of Streptomyces misakiensis [2].
 

High impact information on BE-18257B

  • (Group 2), or after intrarenal infusion of ET-1 superimposed on BE-18257B (Group 3) [3].
  • The present study examined the renal actions of ET-1 after ET-A receptors were blocked by BE-18257B to unmask the functions of ET-B receptors [3].
  • RESULTS: In Group 1, BE-18257B infusion did not alter arterial pressure, renal blood flow (RBF), GFR or tubular function [3].
  • In Group 3, BE-18257B infusion significantly attenuated the decrease in RBF caused by ET-1 and increased GFR by 40% without altering arterial pressure, associated with significant diuresis and natriuresis [3].
  • 8. The ET-1 receptor antagonists, BE-18257B and FR 139317, blocked both the ET-1-induced rise in tone and the potentiation of ATP responses in a concentration-dependent fashion [4].
 

Biological context of BE-18257B

  • CONCLUSION: Renal vasoconstriction caused by ET-1 is attenuated by ET-A receptor blockade with BE-18257B, which unmasks the hemodynamic and tubular actions of ET-B receptors [3].
 

Anatomical context of BE-18257B

 

Associations of BE-18257B with other chemical compounds

 

Gene context of BE-18257B

 

Analytical, diagnostic and therapeutic context of BE-18257B

References

  1. Effects of endothelin-1 and endothelin-A receptor antagonist on recovery after hypothermic cardioplegic ischemia in neonatal lamb hearts. Hiramatsu, T., Forbess, J., Miura, T., Roth, S.J., Cioffi, M.A., Mayer, J.E. Circulation (1995) [Pubmed]
  2. An endothelin receptor (ETA) antagonist isolated from Streptomyces misakiensis. Ihara, M., Fukuroda, T., Saeki, T., Nishikibe, M., Kojiri, K., Suda, H., Yano, M. Biochem. Biophys. Res. Commun. (1991) [Pubmed]
  3. Renal actions of endothelin-1 under endothelin receptor blockade by BE-18257B. Syed, N., Gulmi, F.A., Chou, S.Y., Mooppan, U.M., Kim, H. J. Urol. (1998) [Pubmed]
  4. Involvement of ETA receptors in the facilitation by endothelin-1 of non-adrenergic non-cholinergic transmission in the rat urinary bladder. Donoso, M.V., Salas, C., Sepúlveda, G., Lewin, J., Fournier, A., Huidobro-Toro, J.P. Br. J. Pharmacol. (1994) [Pubmed]
  5. Endothelin-binding inhibitors, BE-18257A and BE-18257B II. Structure determination. Nakajima, S., Niiyama, K., Ihara, M., Kojiri, K., Suda, H. J. Antibiot. (1991) [Pubmed]
  6. Endothelin-binding inhibitors, BE-18257A and BE-18257B. I. Taxonomy, fermentation, isolation and characterization. Kojiri, K., Ihara, M., Nakajima, S., Kawamura, K., Funaishi, K., Yano, M., Suda, H. J. Antibiot. (1991) [Pubmed]
 
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