Antiplatelet activity

Mn2(CO)io in a simple photoinitiated free radical polymerization. The antiplatelet activity of these polymers were compared with that of poly(ether-Wrethane) carrying the hydantoin residues in side chains. 

Many dietary supplements have antiplatelet activity, which may increase the risk of bleeding when used concurrently with anticoagulants. Feverfew inhibits cyclooxygenase and phospholipase A2 and may interact with anticoagulants and potentiate the antiplatelet effect of aspirin. Other supplements that possess antiplatelet activity include but are not limited to garlic, ginkgo, vitamin E, vitamin A, and selenium. 

Thus, Sanofi had two superior and unexpected results that (1) the dextrorotatory enantiomer separated from racemate PCR 4099 contained substantially all of the antiplatelet activity and (2) was essentially devoid of the neurotoxicity associated with PCR 4099. 

Gyclocondensation of diazomalonaldehyde 336 with 4-fluoroaniline carried out in methanol-acetic acid provides l-(4-fluorophenyl)-l,2,3-triazole-l-carbaldehyde 337 in 78% yield. Oxidation with MnOz in the presence of sodium cyanide in methanol converts aldehyde 337 into methyl ester 338 with 79% yield. Hydrazide 339 (84% yield) is obtained in a reaction of ester 338 with hydrazine. Product 339 reacts with various aromatic aldehydes to give hydrazones possessing interesting antiplatelet activity (Scheme 53) <2003BMC2051>. 

Subsequent clinical studies provided additional evidence that GTN exerts antiplatelet activity in vivo and offered insight into the nature of GTN s anti-aggregatory pharmacology. A dose-effect relationship between intravenous GTN and inhibition of platelet aggregation was uncovered in healthy male subjects, in whom plasma... 

Most literature reports of pharmacodynamic botanical-drug interaction involve the anticoagulant warfarin, likely because it has therapeutic end points such as the INR and PT, which are routinely closely monitored. In addition, most botanicals possess anticoagulant and/or antiplatelet activities, and their combined use with warfarin provides a good example of pharmacodynamic interaction with additive pharmacological effect. 

In an effort to investigate antioxidant constituents with antiproliferative effects in rat vascular smooth muscle cells (VSMC), broussoflavan A (36) [49], broussoflavonols F (45) [50] and G (46) [51], and broussoaurone A (48) [49] were found to inhibit the Fe2+-induced thiobarbituric acid-reactive substance formation in rat brain homogenate. Furthermore, broussoflavonols F (45) and G (46) inhibited fetal calf serum-, 5-hydroxytryptamine-, or ADP-induced [3H]thymidine incorporation into rat VSMC [45]. Antioxidant activities and inhibitory effects on proliferation of rat VSMC with potent antiplatelet activities of 45 and 46 may be useful for vascular diseases and atherosclerosis [43,45]. 

Kuo R-Y, Chang F-R, Chen C-Y, Teng C-M, Yen H-F, Wu Y-C (2001) Antiplatelet Activity of N-Methoxycarbonyl Aporphines from Rollinia mucosa. Phytochemistry 57 421... 

Bertelli AA, Giovannini L, Giannessi D, Migliori M, Bernini W, Fregoni M, Bertelli A. 1995. Antiplatelet activity of synthetic and natural resveratrol in red wine. Int J Tissue React 17 1-3. 

ACS represents a prothrombotic state not just confined to the culprit lesion, with evidence of a pan coronary process and generalized platelet activation. Multiple vulnerable plaques in nonculprit vessels have been identified by angioscopy or intravascular ultrasound in ACS. Protracted treatment with clopidogrel induces antiplatelet activity that provides early benefits, and may limit thrombotic events within the following months. In the CURE study, the curves of major vascular events continue to diverge and showed an additional benefit from one-month follow-up to one year. 

As noted earlier, inhibition of PDE leads to the accumulation of intracellular cAMP and cGMR There are also feedback mechanisms—high levels of cAMP may, in turn, have an indirect effect on endogenous factors such as prostacyclin and adenosine, which also serve to further increase the levels of cAMP High levels of cyclic nucleotides have been shown to inhibit platelet aggregation in response to virtually all agonists. However, in the past, the direct antiplatelet activity of dipyridamole has been noted only at very high concentrations, above those usually achieved with oral therapy, and the ability... 

Some of these agents have more than one action, For example, sirolimus is antiproliferative, but also carries antiinflammatory properties and possesses immunoregulatory functions. Similarly, cilastozole has antiplatelet activity, but also inhibits SMC migration and directly inhibits intimal proliferation. Table 2 lists the drugs that have shown positive results in clinical trials and their mechanisms of action. 

Cook JJ, Holahan MA, Lyle EA et al. (1996) Nonpeptide glycoprotein Ilb/IIIa inhibitors. 8. Antiplatelet activity and oral antithrombotic efficacy of L-734,217. J Pharmacol Exp Ther 278 62-73... 

Aspirin a drug that has been used to reduce pain, fever and inflammation. If used for a long time at low doses, it has antiplatelet activity in blood and prevents coagulation. 

ASPIRIN PERIPHERAL VASODILATORS Possible t risk of bleeding with cilostazol. Low-dose aspirin (<80 mg) appears to be safe Additive effect cilostazol has antiplatelet activity Warn the patient to report any signs oft bleeding... 

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