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Chemical Compound Review

Diquafosol     [(2R,3S,4R,5R)-5-(2,4- dioxopyrimidin-1-yl)...

Synonyms: UppppU, INS-365, CHEMBL221326, CHEBI:27791, HMDB06796, ...
 
 
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Disease relevance of UppppU

  • The P2Y2 receptor agonists diuridine tetraphosphate (diquafosol) and the uracil-cytosine dinucleotide denufosol are currently undergoing clinical trials for dry eye disease, retinal detachment disease, upper respiratory tract symptoms, and cystic fibrosis, respectively [1].
  • The percentage of subjects with clearing of foreign body sensation (score of 0) was higher at week 6 in subjects treated with 2% diquafosol (21%) compared with placebo (15%), but the difference did not achieve significance (P=0.193) [2].
 

High impact information on UppppU

  • Significant differences in favor of diquafosol were observed for clearing of foreign body sensation and for worst symptom in secondary data analyses [2].
  • PURPOSE: To investigate the safety and efficacy of diquafosol tetrasodium, a P2Y2 receptor agonist that stimulates fluid and mucin secretion on the ocular surface, as a novel topical treatment of dry eye disease [2].
  • Diquafosol elicits increases in net Cl- transport through P2Y2 receptor stimulation in rabbit conjunctiva [3].
  • The purpose of the present study was to understand the mechanisms of action of diquafosol, a stable derivative of uridine 5'-triphosphate, on Cl(-) transport across the isolated rabbit conjunctiva [3].
  • The ophthalmic formulation of diquafosol tetrasodium (INS365), a P2Y2 receptor agonist, is targeted to treat dry eye disease through rehydration of the ocular surface [4].

References

  1. P2 receptors activated by uracil nucleotides--an update. Brunschweiger, A., Müller, C.E. Current medicinal chemistry. (2006) [Pubmed]
  2. Double-masked, placebo-controlled safety and efficacy trial of diquafosol tetrasodium (INS365) ophthalmic solution for the treatment of dry eye. Tauber, J., Davitt, W.F., Bokosky, J.E., Nichols, K.K., Yerxa, B.R., Schaberg, A.E., LaVange, L.M., Mills-Wilson, M.C., Kellerman, D.J. Cornea (2004) [Pubmed]
  3. Diquafosol elicits increases in net Cl- transport through P2Y2 receptor stimulation in rabbit conjunctiva. Murakami, T., Fujihara, T., Horibe, Y., Nakamura, M. Ophthalmic Res. (2004) [Pubmed]
  4. Diquafosol tetrasodium: a novel dry eye therapy. Nichols, K.K., Yerxa, B., Kellerman, D.J. Expert opinion on investigational drugs. (2004) [Pubmed]
 
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