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Chemical Compound Review

VAPIPROST     (E)-7-[(1R,2R,3S,5S)-3- hydroxy-5-[(4...

Synonyms: Vapiprostum, AC1O5LZK, GR-32191, LS-177875, PDSP2_000517, ...
 
 
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Disease relevance of VAPIPROST

 

High impact information on VAPIPROST

  • Low affinity sites, which irreversibly bind the antagonist GR 32191, transduce platelet activation and aggregation [4].
  • 2. 1-heptan-2-yl-5-heptenoic acid (I-BOP) with high affinity support platelet shape change, whereas low affinity sites that bind irreversibly the antagonist GR 32191 transduce platelet aggregation [5].
  • Blockade of the low affinity TP sites with GR 32191 prevented I-BOP-induced TPalpha phosphorylation [4].
  • To elucidate the respective role of the two classes of pharmacological binding sites of TPs in shape change, platelets were incubated with I-BOP at low concentrations or stimulated by I-BOP at high concentrations after pretreatment with GR 32191 or activated with low concentrations of 8-epi-prostaglandin F(2)alpha [5].
  • 2. Eight prostaglandin E (PGE) analogues were compared against sulprostone for their effects on PAF-induced aggregation in human platelet-rich plasma (PRP) in the presence of GR 32191 and the DP-receptor antagonist, BW A868C [6].
 

Biological context of VAPIPROST

  • The results show that, GR 32191, given orally, in doses of 20 mg and 40 mg, does not reduce the blood pressure to any clinically important degree [2].
 

Anatomical context of VAPIPROST

 

Associations of VAPIPROST with other chemical compounds

  • In contrast to platelets, studies of ligand dissociation only identified GRr sites in rat aortic SMC and GR 32191 failed to inactivate PGH2/TxA2 receptors as detected by the PGH2/TxA2 receptor antagonist, [3H]SQ 29548 [8].
 

Gene context of VAPIPROST

  • The endothelin-1-induced contractions were similarly inhibited by GR 32191 ([1R-[1alpha(Z),2beta,3beta,5alpha]]-(+)-7-[5-([1,1'-b iphenyl]-4-ylmethoxy)-3-hydroxy-2-(1-piperidinyl)cyclopentyl]-4-++ +heptonoic acid, a thromboxane A2 receptor antagonist [9].

References

  1. Ticlopidine prevents renal disease progression in rats with reduced renal mass. Zoja, C., Perico, N., Bergamelli, A., Pasini, M., Morigi, M., Dadan, J., Belloni, A., Bertani, T., Remuzzi, G. Kidney Int. (1990) [Pubmed]
  2. The haemodynamic effects of GR 32191, a thromboxane A2 receptor antagonist, in patients with renal artery stenosis and hypertension. Lyons, D., Fowler, G., Petrie, J.C., Webster, J. British journal of clinical pharmacology. (1993) [Pubmed]
  3. The effect of a thromboxane receptor antagonist on acute ePTFE arterial graft thrombogenicity--an experimental study in sheep. Lundell, A., Bergqvist, D., Leide, S., Lindblad, B., Ljungberg, J. European journal of vascular surgery. (1991) [Pubmed]
  4. Phosphorylation of the thromboxane receptor alpha, the predominant isoform expressed in human platelets. Habib, A., FitzGerald, G.A., Maclouf, J. J. Biol. Chem. (1999) [Pubmed]
  5. Tyrosine phosphorylation of cortactin associated with Syk accompanies thromboxane analogue-induced platelet shape change. Gallet, C., Rosa, J.P., Habib, A., Lebret, M., Lévy-Tolédano, S., Maclouf, J. J. Biol. Chem. (1999) [Pubmed]
  6. Potentiation of aggregation and inhibition of adenylate cyclase in human platelets by prostaglandin E analogues. Matthews, J.S., Jones, R.L. Br. J. Pharmacol. (1993) [Pubmed]
  7. Evidence for thromboxane receptor mediated contraction of guinea-pig and human airways in vitro by prostaglandin (PG) D2, 9 alpha,11 beta-PGF2 and PGF2 alpha. Featherstone, R.L., Robinson, C., Holgate, S.T., Church, M.K. Naunyn Schmiedebergs Arch. Pharmacol. (1990) [Pubmed]
  8. Heterogeneity of prostaglandin H2/thromboxane A2 receptors: distinct subtypes mediate vascular smooth muscle contraction and platelet aggregation. Furci, L., Fitzgerald, D.J., Fitzgerald, G.A. J. Pharmacol. Exp. Ther. (1991) [Pubmed]
  9. Glibenclamide inhibits thromboxane A2-induced contraction in human internal mammary artery and saphenous vein. Stanke, F., Cracowski, J.L., Chavanon, O., Magne, J.L., Blin, D., Bessard, G., Devillier, P. Eur. J. Pharmacol. (1998) [Pubmed]
 
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