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Chemical Compound Review:

AG-K-56770 (3R,6S,11S,14S,20S,23S)-6- acetamido-3...

Synonyms: MK-0852, KST-1A1805, CTK0H9338, AR-1A6968, MK 852, ...

Ramjit, D.R. et al., Greenberg, H.E. et al., Kingma, J.G. et al., May, J.A. et al., Wittig, K. et al., et al.

Kingma, Plante, Bogaty,

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Disease relevance of MK 852

OBJECTIVES: We studied the effects of N-acetyl-cys-asn-(5,5-dimethyl-4-thiazolidine-carbonyl)-4-amino-methyl-phe-gly-asp-cys, monoacetate (MK-0852) (platelet GPIIb/IIIa receptor blocker) on peak reactive hyperemia, distribution of blood flow, regional contractile function and infarct size in a canine model of acute ischemia-reperfusion injury [1].
Antithrombotic effects of MK-0852, a platelet fibrinogen receptor antagonist, in canine models of thrombosis [2].

High impact information on MK 852

Therefore, in this study effects of MK-852, a cyclic hexapeptide based on the RGD-template, on the platelet phenotype were analysed by whole blood flow cytometry [3].
In a canine model of electrically induced LCX coronary artery thrombosis, i.v. MK-0852 (100 micrograms/kg + 3 micrograms/kg/min), initiated 15 min before the initiation of electrical injury, prevented occlusive thrombosis in 4 of 6 preparations despite the continued electrical stimulation of the vessel for 180 min [2].
The i.v. infusion of 1.0 and 3.0 micrograms/kg/min MK-0852 to anesthetized dogs significantly inhibited ex vivo platelet aggregation responses to ADP and collagen, with the 3.0 micrograms/kg/min infusion completely inhibiting ex vivo aggregation responses to both agonists [2].
The pharmacokinetics of MK-852 include an elimination half-life of approximately 2 hours, total clearance of about 150 ml/min, and volume of distribution of about 18 liters [4].
At infusion rates of 1 microgram/kg/min for 1 hour and 0.44 microgram/kg/min for 4 hours, respectively, MK-852 extended baseline bleeding time by greater than 2.2-fold and 2.6-fold, inhibited ADP-induced platelet aggregation by 76% and 69%, and inhibited collagen-induced platelet aggregation by 65% and 67%, respectively [4].

Anatomical context of MK 852

The i.v. administrations of 100 and 300 micrograms/kg MK-0852 suppressed platelet-dependent cyclic flow reductions in stenosed canine left circumflex (LCX) coronary artery for periods of 24 +/- 3 and 64 +/- 4 min, respectively [2].
Changes in the composition of the platelet cytoskeleton in response to ADP: effects of MK-852 and ARL 66096 [5].
The Asp/Dip/AR-C was superior to abciximab and MK-852 in inhibiting platelet and leukocyte function [6].

Gene context of MK 852

Likewise, aggregation was inhibited by the anti-GPIIb/IIIa antibody MA-16N7C2 and by the GPIIb/IIIa antagonists G4120 or MK-852 [7].
As with MK-852, myosin incorporation became reversible [5].
In the presence of MK-852 there was no increase in ABP or the 66K protein and no decrease in the 31K protein [5].

Analytical, diagnostic and therapeutic context of MK 852

Determination of MK-852, a new fibrinogen receptor antagonist, in plasma and urine by radioimmunoassay [8].

References

Platelet GPIIb/IIIa receptor blockade reduces infarct size in a canine model of ischemia-reperfusion. Kingma, J.G., Plante, S., Bogaty, P. J. Am. Coll. Cardiol. (2000) [Pubmed]
Antithrombotic effects of MK-0852, a platelet fibrinogen receptor antagonist, in canine models of thrombosis. Ramjit, D.R., Lynch, J.J., Sitko, G.R., Mellott, M.J., Holahan, M.A., Stabilito, I.I., Stranieri, M.T., Zhang, G., Lynch, R.J., Manno, P.D. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
Inhibition of fibrinogen binding and surface recruitment of GpIIb/IIIa as dose-dependent effects of the RGD-mimetic MK-852. Wittig, K., Rothe, G., Schmitz, G. Thromb. Haemost. (1998) [Pubmed]
Antiplatelet effects of MK-852, a platelet fibrinogen receptor antagonist, in healthy volunteers. Greenberg, H.E., Wissel, P., Barrett, J., Barchowsky, A., Gould, R., Farrell, D., Panebianco, D., Hand, E., Gillen, L., Goldberg, M.R., Bjornsson, T.D. Journal of clinical pharmacology. (2000) [Pubmed]
Changes in the composition of the platelet cytoskeleton in response to ADP: effects of MK-852 and ARL 66096. May, J.A., Heptinstall, S., Spangenberg, P. Blood Coagul. Fibrinolysis (1996) [Pubmed]
The effects of GPIIb-IIIa antagonists and a combination of three other antiplatelet agents on platelet-leukocyte interactions. Zhao, L., Bath, P.M., Fox, S., May, J., Judge, H., Lösche, W., Heptinstall, S. Current medical research and opinion. (2003) [Pubmed]
Dose-responses to inducers and inhibitors of platelet aggregation analysed via a micro-method. Hoylaerts, M.F., Thys, C., Stassen, J.M., Vermylen, J. Blood Coagul. Fibrinolysis (1996) [Pubmed]
Determination of MK-852, a new fibrinogen receptor antagonist, in plasma and urine by radioimmunoassay. Yuan, A.S., Hand, E.L., Hichens, M., Olah, T.V., Barrish, A., Fernandez-Metzler, C., Gilbert, J.D. Journal of pharmaceutical and biomedical analysis. (1993) [Pubmed]

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