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Chemical Compound Review:

Aspalatone (2-methyl-4-oxo-pyran-3-yl) 2...

Synonyms: BK-111, LS-35537, ZINC00006255, AC1L53AE, 147249-33-0, ...

Suh, D.Y. et al., Kim, H.C. et al., Han, B.H. et al., Gwak, H.S. et al., Suh, D.Y. et al.

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High impact information on Aspalatone

The antioxidant efficacy of aspalatone (APT; acetyl salicylic acid maltol ester), a new antiplatelet agent, has been characterized in vivo as well as in vitro, and several observations indicated that the antioxidant could prevent the neuroexcitation caused by oxidative stress [1].
Effect of vehicles and enhancers on the in vitro skin penetration of aspalatone and its enzymatic degradation across rat skins [2].
Both aspalatone and ASA were essentially stable in gastric juice and were absorbed in stomach unchanged [3].
In in vitro experiments with rat serum, intestinal fluid, liver and gastric mucosal homogenates, SM was the only compound formed after 4 min incubation at 37 degrees C. From these results it was concluded that aspalatone does not behave as a prodrug of ASA in rats [4].
In order to determine whether aspalatone ([3-(2-methyl-4-pyronyl)]-2- acetyloxybenzoate, CAS 147249-33-0), a new antiplatelet agent, behaves as a prodrug of acetylsalicylic acid (ASA), metabolism studies in rats were carried out in vivo and in vitro using the whole animal and tissue homogenates [4].

Biological context of Aspalatone

The ability of oral aspalatone to inhibit platelet aggregation in rats ex vivo was compared with other reference antiplatelet drugs [5].

Gene context of Aspalatone

In addition, the results of experiments using certain esterase inhibitors, suggested the major contribution of B-esterase(s) in the metabolism of aspalatone to SM particularly in serum and intestinal fluid [4].

References

Aspalatone, a new antiplatelet agent, attenuates the neurotoxicity induced by kainic acid in the rat. Kim, H.C., Choi, D.Y., Jhoo, W.K., Lee, D.W., Koo, C.H., Kim, C. Life Sci. (1997) [Pubmed]
Effect of vehicles and enhancers on the in vitro skin penetration of aspalatone and its enzymatic degradation across rat skins. Gwak, H.S., Chun, I.K. Arch. Pharm. Res. (2001) [Pubmed]
Salicylate levels in rat stomach tissues after administration of aspalatone and acetylsalicylic acid in relation to their ulcerogenicity. Suh, D.Y., Kang, Y.H., Han, B.H. Arzneimittel-Forschung. (1997) [Pubmed]
Metabolic fate of the new antithrombotic agent aspalatone in rats. In vivo and in vitro study. Suh, D.Y., Yang, H.O., Kim, Y.C., Han, B.H. Arzneimittel-Forschung. (1995) [Pubmed]
Synthesis and antiplatelet effects of the new antithrombotic agent aspalatone with low ulcerogenicity. Han, B.H., Suh, D.Y., Yang, H.O., Park, Y.H., Kang, Y.H., Kim, Y.C. Arzneimittel-Forschung. (1994) [Pubmed]

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