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Chemical Compound Review

SureCN9117189     methyl[(2R)-1- (octadecylcarbamoyloxy)-3...

Synonyms: AC1L2VH6, Ro 193704, Ro 19-3704, 106556-34-7
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Disease relevance of methyl [(1R)-1-(stearylcarbamoyloxymethyl)-2-(4-thiazol-3-ylbutoxy)ethyl] carbonate

 

High impact information on methyl [(1R)-1-(stearylcarbamoyloxymethyl)-2-(4-thiazol-3-ylbutoxy)ethyl] carbonate

  • PAF analog, RO 19-3704, which is a PAF-receptor antagonist, inhibited RGC secretion mediated by PAF in a dose-dependent manner with an inhibitory concentration of 50% of 70 ng/ml [2].
  • Competitive inhibition of phospholipase A2 activity by the platelet-activating factor antagonist Ro 19-3704 and evidence for a novel suppressive effect on platelet activation [3].
  • The compound Ro 19-3704 [3-4(R)-2-(methoxycarbonyl) oxy-3-(octadecylcarbamoyl)oxy-propoxy butylthiazolium iodide], initially described as an antagonist of platelet-activating factor, is reported here to directly inhibit rabbit platelet phospholipase (PL) A2 activity, with an IC50 value of 4 to 7 microM [3].
  • 3. Experiments on plasma membrane preparations showed that Ro 19-3704 inhibited [3H]-yohimbine binding with an inhibition constant (Ki) of 7 +/- 3 microM [4].
  • 4. Administered intravenously, Ro 19-3704 failed to block bronchoconstriction induced by an i.v. injection of ovalbumin to guinea-pigs passively sensitized with anti-ovalbumin antiserum [1].
 

Anatomical context of methyl [(1R)-1-(stearylcarbamoyloxymethyl)-2-(4-thiazol-3-ylbutoxy)ethyl] carbonate

  • Ro 18-7715, another Paf antagonist and analogue of Ro 19-3704, failed to inhibit the production of superoxide anions by macrophages stimulated by FMLP at concentrations which were effective against Paf [1].
 

Gene context of methyl [(1R)-1-(stearylcarbamoyloxymethyl)-2-(4-thiazol-3-ylbutoxy)ethyl] carbonate

  • It is inhibited by equimolar concentrations of the potent PAF-receptor antagonist, Ro 19-3704 [5].
  • PAF caused a dose-dependent increase in RGC release in concentrations ranging from 100-0.5 microM during a 1-2 hours incubation with either feline or human explants, and the effect was inhibited by the PAF receptor antagonists Ro 19-3704 [6].

References

  1. Interference of the Paf antagonist Ro 19-3704 with Paf and antigen-induced bronchoconstriction in the guinea-pig. Lagente, V., Desquand, S., Hadvary, P., Cirino, M., Lellouch-Tubiana, A., Lefort, J., Vargaftig, B.B. Br. J. Pharmacol. (1988) [Pubmed]
  2. Platelet-activating factor stimulates secretion of respiratory glycoconjugate from human airways in culture. Goswami, S.K., Ohashi, M., Stathas, P., Marom, Z.M. J. Allergy Clin. Immunol. (1989) [Pubmed]
  3. Competitive inhibition of phospholipase A2 activity by the platelet-activating factor antagonist Ro 19-3704 and evidence for a novel suppressive effect on platelet activation. Mounier, C., Hatmi, M., Faili, A., Bon, C., Vargaftig, B.B. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
  4. Selective inhibition of adrenaline-induced human platelet aggregation by the structurally related Paf antagonist Ro 19-3704. Schattner, M., Parini, A., Fouque, F., Vargaftig, B.B., Touqui, L. Br. J. Pharmacol. (1989) [Pubmed]
  5. Platelet activating factor stimulates secretion of mucin by explants of rodent airways in organ culture. Adler, K.B., Schwarz, J.E., Anderson, W.H., Welton, A.F. Exp. Lung Res. (1987) [Pubmed]
  6. Platelet activating factor and tracheobronchial respiratory glycoconjugate release in feline and human explants: involvement of the lipoxygenase pathway. Lundgren, J.D., Kaliner, M., Logun, C., Shelhamer, J.H. Agents Actions (1990) [Pubmed]
 
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