Nitric oxide (NO) is a potent inhibitor of platelet aggregation upon platelet activation by various agonists.Many drugs may influence platelet function both via the L-Arg/NO and the AA/COX-1 pathway.Acetyl group donors, acetoxy drugs, such as DAMC (7,8-diacetoxy-4-methylcoumarin), have recently been reported to activate human platelet NOS via calreticulin transacetylase.Acetylsalicylic acid (O-acetylsalicylic acid, ASA) is well-known to inhibit irreversibly COX-1 activity by O-acetylating a certain serine moiety of the catalytic site of the enzyme.We, therefore, tested three ASA derivatives (O-acetylsalicylic acid cysteine ethylester (ASA-CysEt), di-O-acetylsalicylic acid cysteine Et ester (di-ASA-CysEt) and guaimesal) for an inhibitory action on the activity of a recombinant bovine COX-1 and of endogenous COX-1 in human platelets.ASA-CysEt and di-ASA-CysEt inhibited the activity of recombinant bovine COX-1 albeit to a different degree.Guaimesal was found to be as potent as ASA in inhibiting aggregation and thromboxane synthesis in human platelets.

01 May 1998·Journal of Chromatography B: Biomedical Sciences and Applications

Gas chromatographic–tandem mass spectrometric determination of acetylsalicylic acid in human plasma after oral administration of low-dose aspirin and guaimesal

Article

Author: Jürgen C Frölich ; Joachim Greipel ; Dimitrios Tsikas ; Kathrin S Tewes ; Frank-Mathias Gutzki ; Edzard Schwedhelm

A fully validated gas chromatographic-tandem mass spectrometric (GC-MS-MS) method is described for the accurate determination of acetylsalicylic acid (ASA) in human plasma after a single low-dose oral administration of aspirin or guaimesal, an ASA releasing prodrug. ASA and the newly prepared O-[2H3]-acetylsalicylic acid (d3-ASA) used as internal standard were determined in 100-microl aliquots of plasma by extractive pentafluorobenzyl (PFB) esterification using PFB bromide and tetrabutylammoniumhydrogen sulphate as the esterifying and ion-pairing agent, respectively, and by GC-MS-MS analysis in the negative-ion chemical ionization mode. The overall relative standard deviations were below 8% for ASA levels in the range 0-1 microg/ml plasma. Mean accuracy was 3.8% for ASA levels within the range 0-100 ng/ml. The limit of quantitation of the method was determined as 200 pg/ml ASA at an accuracy of 5.5% and a precision of 15.2%. The limit of detection was determined as 546 amol of ASA at a signal-to-noise ratio of 10:1.

30 Sep 1984·La Clinica terapeutica

[Guaimesal capsules in the treatment of exacerbated chronic bronchitis].

Article

Author: Ghiringhelli, G

100 Deals associated with Guaimesal

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