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Chemical Compound Review

Org-9935     6-(5,6- dimethoxybenzothiophen-2-yl)- 5...

Synonyms: CHEMBL2074862, SureCN4943014, AC1L2YKU, Org 9935, 129425-83-8
 
 
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High impact information on Org 9935

  • This study evaluated the impact of meiosis arrest by PDE3 inhibitor, Org 9935, on developmental competence of geminal vesicle (GV)-stage oocytes from small antral follicles [1].
  • Making use of a selective PDE 3 inhibitor, Org 9935 (10 microM), oocytes retrieved from immature follicles were arrested in prophase I with a high efficiency for up to 72 h [2].
  • 4 PDE IV-selective (rolipram), PDE III-selective (Org 9935) and dual PDE III/IV (Org 30029) inhibitors were effective relaxants of human bronchial smooth muscle [3].
  • Infiltration of lymphocytes and macrophages was significantly inhibited by Org 9935 only (P<0.05 and P<0.01, respectively), whereas neutrophil influx was not significantly affected [4].
  • Although the shape of the concentration-inhibition curve for Org 30029 precluded estimation of an IC50 value, this drug was clearly much less potent than Org 9935 (IC50 about 50 nM) in inhibiting islet phosphodiesterase activity [5].

References

  1. Effect of phosphodiesterase type 3 inhibitor on developmental competence of immature mouse oocytes in vitro. Nogueira, D., Cortvrindt, R., De Matos, D.G., Vanhoutte, L., Smitz, J. Biol. Reprod. (2003) [Pubmed]
  2. Human oocytes reversibly arrested in prophase I by phosphodiesterase type 3 inhibitor in vitro. Nogueira, D., Albano, C., Adriaenssens, T., Cortvrindt, R., Bourgain, C., Devroey, P., Smitz, J. Biol. Reprod. (2003) [Pubmed]
  3. Human bronchial cyclic nucleotide phosphodiesterase isoenzymes: biochemical and pharmacological analysis using selective inhibitors. de Boer, J., Philpott, A.J., van Amsterdam, R.G., Shahid, M., Zaagsma, J., Nicholson, C.D. Br. J. Pharmacol. (1992) [Pubmed]
  4. Bronchodilatory and anti-inflammatory properties of inhaled selective phosphodiesterase inhibitors in a guinea pig model of allergic asthma. Santing, R.E., de Boer, J., Rohof, A., van der Zee, N.M., Zaagsma, J. Eur. J. Pharmacol. (2001) [Pubmed]
  5. The effect of selective phosphodiesterase inhibitors on plasma insulin concentrations and insulin secretion in vitro in the rat. El-Metwally, M., Shafiee-Nick, R., Pyne, N.J., Furman, B.L. Eur. J. Pharmacol. (1997) [Pubmed]
 
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