Description | Azaindole1(TC-S7001)isaselectiveRho-associatedproteinkinase(ROCK)inhibitorwithIC50of0.6and1.1 nMforhumanROCK-1andROCK-2inanATP-competitivemanner. | ||||
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Invitro | Azaindole1inducesvasorelaxationinvitro.Azaindole1inhibitsconcentrationdependentlythephenylephrine-inducedcontractionofrabbitsaphenousarterywithanIC50valueof65 nm.[1] | ||||
Invivo | Azaindole1inducedadose-dependentandlong-lastingdecreaseinbloodpressureinanaesthetizednormotensiverats.i.v.admiNISTrationof0.03,0.1,0.3 mg kg−1,resultedinareductioninthemaximalbloodpressureof8,18,35 mmHg,respectively.Innormotensiverats,azaindole1alsoinducedadose-dependentandpersistentdecreaseinbloodpressure.Inconsciousspontaneouslyhypertensiverats,azaindole1inducedadose-dependentandlong-lastingdecreaseinmeanbloodpressureafteroralapplication.Atalldosestested,azaindole1causesonlyamoderateanddose-independentincreaseinheartrate.[1] |