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Chemical Compound Review:

Mergepta 2-[2- (diaminomethylideneamino) ethylsulfany...

Synonyms: Mergetpa, AG-L-65449, CTK8D5675, AR-1E5742, LS-177336, ...

Püschel, G.P. et al., Proud, D. et al., Palmieri, F.E. et al., Björkman, J.A. et al., Schaffel, R. et al.

Björkman, Abrahamsson, Nerme, Mattsson,

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Disease relevance of Mergetpa

The efficacy of rt-PA alone, or in combination with the carboxypeptidase inhibitor MERGETPA, was compared in a dog model of coronary artery thrombosis [1].

High impact information on Mergetpa

The nasal carboxypeptidase was activated 475% by 0.1 mM CoCl2 and was inhibited by the carboxypeptidase N inhibitor, MERGETPA (D-L-mercaptomethyl-3-guanidino-ethylthiopropanoic acid) (IC50 = 10 microM) [2].
The carboxypeptidase N inhibitor MERGETPA (D-L-mercaptoethanol-3-guanidino-ethylthiopropanoic acid) inhibited the plasma membrane bound carboxypeptidase with an I50 of 0.3 microM [3].
3) The elimination of C3a plus C3adesArg immunoreactivity during a single liver passage was around 67%, irrespective of the perfusion direction and the presence of the carboxypeptidase inhibitor MERGETPA; however, less C3adesArg and more intact C3a appeared in the perfusate in the presence of MERGETPA in orthograde and retrogade perfusions [4].
In rat duodenum, an almost complete blockade of kininase activity was achieved when bacitracin and mergetpa were used together with enalaprilat [5].

References

Inhibition of carboxypeptidase U (TAFIa) activity improves rt-PA induced thrombolysis in a dog model of coronary artery thrombosis. Björkman, J.A., Abrahamsson, T.I., Nerme, V.K., Mattsson, C.J. Thromb. Res. (2005) [Pubmed]
Kinin metabolism in human nasal secretions during experimentally induced allergic rhinitis. Proud, D., Baumgarten, C.R., Naclerio, R.M., Ward, P.E. J. Immunol. (1987) [Pubmed]
Kinin and enkephalin conversion by an endothelial, plasma membrane carboxypeptidase. Palmieri, F.E., Bausback, H.H., Churchill, L., Ward, P.E. Biochem. Pharmacol. (1986) [Pubmed]
Differential effects of human anaphylatoxin C3a on glucose output and flow in rat liver during orthograde and retrograde perfusion: the periportal scavenger cell hypothesis. Püschel, G.P., Oppermann, M., Neuschäfer-Rube, F., Götze, O., Jungermann, K. Biochem. Biophys. Res. Commun. (1991) [Pubmed]
Potentiation of bradykinin effects and inhibition of kininase activity in isolated smooth muscle. Schaffel, R., Rodrigues, M.S., Assreuy, J. Can. J. Physiol. Pharmacol. (1991) [Pubmed]

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