生物活性CapromorelinTartrate是一種可口服的,有效的growthhormonesecretagoguereceptor(GHSR)激動(dòng)劑,對hGHS-R1a的Ki值為7nM。靶點(diǎn)Ki:7nM(hGHS-R1a)體外研究CapromorelinstimulatesGHreleaseinratpituitarycellcultureswithEC50of3nM.體內(nèi)研究Dogsreceivingcapromorelin(30mg/mL)havefoodconsumptionthatissignificantlygreaterthandogstreatedwithplacebo.Alldogsinthecapromorelingroupgainweightby0.52kg,morethanthatofplacebogroup.Capromorelinshowsenhancedintestinalabsorptioninrodentmodelsandexhibitssuperiorpharmacokineticproperties,includinghighbioavailabilitiesintwoanimalspecies[F(rat)=65%,F(dog)=44%].CapromorelinstimulatesGHreleaseinanesthesizedratmodel,withED50of0.05mg/kgiv.
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