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Chemical Compound Review

DMP728     (4R,7S,13R)-7-[3- (diaminomethylideneamino)...

Synonyms: XL118, LS-173477, AC1L3TI7, C25H36N8O7.CH4O3S
This record was replaced with 121845.
 
 
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Disease relevance of (5R,11S,14R)-14-ethyl-11-(3-guanidinopropyl)-12-methyl-4,7,10,13,16-pentaoxo-3,6,9,12,15-pentazabicyclo[15.3.1]henicosa-17,19,21-triene-5-carboxylic acid

  • The goals of the present study were to determine the oral antiplatelet and antithrombotic efficacies of DMP 728 in various arterial thrombosis models in dogs [1].
 

High impact information on (5R,11S,14R)-14-ethyl-11-(3-guanidinopropyl)-12-methyl-4,7,10,13,16-pentaoxo-3,6,9,12,15-pentazabicyclo[15.3.1]henicosa-17,19,21-triene-5-carboxylic acid

  • DMP 728 effects on bleeding time prolongation could be reversed more rapidly than those on platelet aggregation inhibition [1].
  • CONCLUSIONS: These data suggest that DMP 728, a low-molecular-weight GPIIb/IIIa receptor antagonist, may have therapeutic potential as an oral antithrombotic agent in coronary and carotid artery thromboembolic disorders [1].
  • In the coronary artery Folts' model in dogs, DMP 728 demonstrated maximal antithrombotic efficacy at 0.01 mg/kg IV and < 0.6 mg/kg PO [1].
  • DMP 728 demonstrated dose-dependent oral antiplatelet effects with an absolute oral bioavailability of 8% to 12% in dogs [1].
  • METHODS AND RESULTS: DMP 728 demonstrated antiplatelet efficacy in vitro in inhibiting ADP-induced human platelet aggregation (IC50, 46 +/- 2 nmol/L) and fibrinogen binding to human platelets (IC50, 2.3 +/- 0.8 nmol/L) or purified human GPIIb/IIIa receptors (IC50, 0.6 +/- 0.1 nmol/L) [2].
 

Chemical compound and disease context of (5R,11S,14R)-14-ethyl-11-(3-guanidinopropyl)-12-methyl-4,7,10,13,16-pentaoxo-3,6,9,12,15-pentazabicyclo[15.3.1]henicosa-17,19,21-triene-5-carboxylic acid

  • In vivo antithrombotic efficacy of GPIIb/IIIa receptor antagonists (m7E3, MK-383 and DMP-728) was studied with respect to their ex vivo platelet inhibition in heparinized platelet-rich plasma (hPRP) and citrated platelet-rich plasma (cPRP) using a canine model of carotid artery thrombosis [3].
 

Biological context of (5R,11S,14R)-14-ethyl-11-(3-guanidinopropyl)-12-methyl-4,7,10,13,16-pentaoxo-3,6,9,12,15-pentazabicyclo[15.3.1]henicosa-17,19,21-triene-5-carboxylic acid

  • Pharmacodynamics and pharmacokinetics of DMP 728, a platelet GPIIb/IIIa antagonist, in healthy subjects [4].
  • PURPOSE: The purpose of this study was to test whether structural modifications improve the intestinal absorption of DMP 728 (cyclo(D-Abu-NMeArg-Gly-Asp-Amb)), a GPIIb/IIIa receptor antagonist [5].
  • The effect of absorption enhancers on the oral absorption of the GP IIB/IIIA receptor antagonist, DMP 728, in rats and dogs [6].
  • At all of the above regimens, DMP 728 did not result in any significant effects on platelet counts [7].
 

Anatomical context of (5R,11S,14R)-14-ethyl-11-(3-guanidinopropyl)-12-methyl-4,7,10,13,16-pentaoxo-3,6,9,12,15-pentazabicyclo[15.3.1]henicosa-17,19,21-triene-5-carboxylic acid

 

Associations of (5R,11S,14R)-14-ethyl-11-(3-guanidinopropyl)-12-methyl-4,7,10,13,16-pentaoxo-3,6,9,12,15-pentazabicyclo[15.3.1]henicosa-17,19,21-triene-5-carboxylic acid with other chemical compounds

  • Two other analogs with improved permeability were linear Ac-D-Abu-NMeArg-Gly-Asp-Amb and a DMP 728 derivative in which the Asp was rearranged [5].
  • An automated ion exchange solid phase extraction (IX-SPE) procedure was developed to selectively extract the seven metabolites of roxifiban and its deuterated internal standard while specifically excluding DMP 728 [9].
  • DMP 728, cyclo (D-2-aminobutyrate-N-Methyl-L-Arginyl-Glycyl-L-Aspartyl- 3-amino-methyl-benzoic acid) methanesulfonate salt, is a novel antiplatelet agent with high affinity and specificity for human and canine platelet GPIIb/IIIa (alpha 2/beta 3) receptors [7].
 

Gene context of (5R,11S,14R)-14-ethyl-11-(3-guanidinopropyl)-12-methyl-4,7,10,13,16-pentaoxo-3,6,9,12,15-pentazabicyclo[15.3.1]henicosa-17,19,21-triene-5-carboxylic acid

  • Antiplatelet and antithrombotic efficacy of DMP 728, a novel platelet GPIIb/IIIa receptor antagonist [2].
  • DC11 was chosen for in vivo evaluation based on its ability to inhibit the binding of [3H]DMP 728 to activated platelets and to attenuate the inhibition of ADP-induced aggregation on platelet-rich plasma ex vivo by DMP 728 [8].
  • The IC50 of DMP 728 in inhibiting human platelet aggregation in PRP ranged from 0.02-0.05 microM regardless of the agonist used or even their combinations [7].
 

Analytical, diagnostic and therapeutic context of (5R,11S,14R)-14-ethyl-11-(3-guanidinopropyl)-12-methyl-4,7,10,13,16-pentaoxo-3,6,9,12,15-pentazabicyclo[15.3.1]henicosa-17,19,21-triene-5-carboxylic acid

References

  1. Oral antiplatelet, antithrombotic efficacy of DMP 728, a novel platelet GPIIb/IIIa antagonist. Mousa, S.A., DeGrado, W.F., Mu, D.X., Kapil, R.P., Lucchesi, B.R., Reilly, T.M. Circulation (1996) [Pubmed]
  2. Antiplatelet and antithrombotic efficacy of DMP 728, a novel platelet GPIIb/IIIa receptor antagonist. Mousa, S.A., Bozarth, J.M., Forsythe, M.S., Jackson, S.M., Leamy, A., Diemer, M.M., Kapil, R.P., Knabb, R.M., Mayo, M.C., Pierce, S.K. Circulation (1994) [Pubmed]
  3. Correlation between the in vivo efficacy of GPIIb/IIIa receptor antagonists (m7E3, MK-383 and DMP-728) and ex vivo platelet inhibition. Huang, J., Rebello, S.S., Faul, J.D., Lucchesi, B.R. Pharmacology (1999) [Pubmed]
  4. Pharmacodynamics and pharmacokinetics of DMP 728, a platelet GPIIb/IIIa antagonist, in healthy subjects. Michaelis, W., Turlapaty, P., Gray, J., Fiske, W.D., Faulkner, E., Kornhauser, D., Mousa, S.A. Clin. Pharmacol. Ther. (1998) [Pubmed]
  5. Prodrug and analog approaches to improving the intestinal absorption of a cyclic peptide, GPIIb/IIIa receptor antagonist. Saitoh, H., Aungst, B.J. Pharm. Res. (1997) [Pubmed]
  6. The effect of absorption enhancers on the oral absorption of the GP IIB/IIIA receptor antagonist, DMP 728, in rats and dogs. Burcham, D.L., Aungst, B.A., Hussain, M., Gorko, M.A., Quon, C.Y., Huang, S.M. Pharm. Res. (1995) [Pubmed]
  7. Intravenous antiplatelet efficacy and safety of the platelet GPIIb/IIIa antagonist, DMP 728 in anesthetized dogs. Mousa, S.A., Flint, S., Lorelli, W., Hassell, S., Bozarth, J., De Grado, W., Reilly, T.M. Thromb. Res. (1994) [Pubmed]
  8. A monoclonal antibody that recognizes the GPIIb/IIIa antagonist DMP 728. Reversal of the effects of DMP 728 on platelet aggregation and bleeding time in the dog. Reilly, T.M., Mousa, S.A., Racanelli, A.L., Thoolen, M.J., Flint, S.K., Bozarth, J.M., Mu, D.X., Walton, H.L. Arterioscler. Thromb. Vasc. Biol. (1995) [Pubmed]
  9. Simultaneous quantification of seven active metabolites of roxifiban in human plasma by LC/MS/MS in the presence of an interfering displacer at millimolar concentrations. Shi, G., Lloyd, T.L., Sy, S.K., Jiao, Q., Wernicki, A., Mutlib, A., Emm, T.A., Unger, S.E., Pieniaszek, H.J. Journal of pharmaceutical and biomedical analysis. (2003) [Pubmed]
  10. Platelet GPIIb/IIIa receptor occupancy studies using a novel fluoresceinated cyclic Arg-Gly-Asp peptide. Tsao, P.W., Bozarth, J.M., Jackson, S.A., Forsythe, M.S., Flint, S.K., Mousa, S.A. Thromb. Res. (1995) [Pubmed]
  11. Determination of DMP 728, a IIb/IIIa receptor antagonist, in rat and dog plasma by high-performance liquid chromatography with fluorimetric detection. Wu, S.T., Stampfli, H.F., Banks, C.M., Emm, T.A., Kapil, R.P., Padovani, P.K., Lee, W.M., Huang, S.M. J. Chromatogr. B, Biomed. Appl. (1994) [Pubmed]
 
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