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Literature summary for 3.4.21.68 extracted from

  • David, H.N.; Haelewyn, B.; Risso, J.J.; Colloch, N.; Abraini, J.H.
    Xenon is an inhibitor of tissue-plasminogen activator: adverse and beneficial effects in a rat model of thromboembolic stroke (2010), J. Cereb. Blood Flow Metab., 30, 718-728.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.21.68

Application

Application Comment Organism
medicine therapy for acute ischemic stroke Rattus norvegicus
medicine therapy for acute ischemic stroke Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
xenon intraischemic xenon dose-dependently inhibits tissue-type plasminogen activator-induced thrombolysis and subsequent reduction of ischemic brain damage, postischemic xenon virtually suppresses ischemic brain damage and tissue-type plasminogen activator-induced brain hemorrhages and disruption of the blood-brain barrier, therefore xenon should not be administered before or together with a tissue-type plasminogen activator therapy Homo sapiens
xenon intraischemic xenon dose-dependently inhibits tissue-type plasminogen activator-induced thrombolysis and subsequent reduction of ischemic brain damage, postischemic xenon virtually suppresses ischemic brain damage and tissue-type plasminogen activator-induced brain hemorrhages and disruption of the blood-brain barrier, therefore xenon should not be administered before or together with a tissue-type plasminogen activator therapy Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Homo sapiens P00750
-
-
Rattus norvegicus
-
 Sprague-Dawley rat
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation actilyse Rattus norvegicus
-
commercial preparation actilyse Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
methylsulfonyl-D-cyclohexylglycyl-Arg-7-amido-4-methylcoumarin + H2O chromogenic substrate Rattus norvegicus methylsulfonyl-D-cyclohexylglycyl-Arg + 7-amino-4-methylcoumarin
-
 ?
methylsulfonyl-D-cyclohexylglycyl-Arg-7-amido-4-methylcoumarin + H2O chromogenic substrate Homo sapiens methylsulfonyl-D-cyclohexylglycyl-Arg + 7-amino-4-methylcoumarin
-
 ?

Synonyms

Synonyms Comment Organism
Alteplase
-
 Rattus norvegicus
Alteplase
-
 Homo sapiens
Tissue-type plasminogen activator
-
 Rattus norvegicus
Tissue-type plasminogen activator
-
 Homo sapiens
tPA
-
 Rattus norvegicus
tPA
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Rattus norvegicus
37
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
 although xenon at 25% (v/v) has no effect, xenon at higher concentrations of 37.5, 50 and 75% inhibit the catalytic efficiencies of human enzyme, IC50 is 34.85% (v/v) Homo sapiens xenon
additional information
-
 although xenon at 25% (v/v) has no effect, xenon at higher concentrations of 37.5, 50 and 75% inhibit the catalytic efficiencies of murine enzyme, IC50 is 37.39% (v/v) Rattus norvegicus xenon

General Information

General Information Comment Organism
physiological function serine protease Rattus norvegicus
physiological function serine protease Homo sapiens