Description | JNJ-42153605isapotentandselectivemGlu2receptorpositiveallostericmodulatorwithanEC50of17nM. | ||
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Targets |
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Invitro | JNJ-42153605isfoundtonothaveagoNISTorantagonistactivitytowardothermGlureceptorsubtypesupto30μM(>50-foldvsmGluR2)andalsoshowsnoornegligIBLeaffinityoractivityatanyofthetargetsintheCEREPpanelofreceptors(>100-foldselectivityformGlu2receptor)[1]. | ||
Invivo | Inmice,JNJ-42153605dose-dependentlyandsignificantlyattenuatestheincreaseinlocomotoractivityinducedbyphencyclidine(PCP,5mg/kgsc)withanED50of5.4mg/kgsc.JNJ-42153605showsarapidrateofabsorptionfromthegastrointestinaltract,reachingthemaximalconcentrationafter0.5h.Clearanceinvivoismoderatetohighinbothratanddog(35and29mL/min/kg,respectively).Eliminationhalflivesareontheshortersideacrossthespecies,being2.7hinratand0.8−1.1hindog.Volumeofdistributionisslightlyhigherthantotalbodywater,indicatingdistributionoutsidetheplasma.BioavailABIlityislowtomoderateacrossthespecies(35%inratand18−33%indog)[1]. |