生物活性CapromorelinTartrate是一种可口服的,有效的growthhormonesecretagoguereceptor(GHSR)激动剂,对hGHS-R1a的Ki值为7nM。靶点Ki:7nM(hGHS-R1a)体外研究CapromorelinstimulatesGHreleaseinratpituitarycellcultureswithEC50of3nM.体内研究Dogsreceivingcapromorelin(30mg/mL)havefoodconsumptionthatissignificantlygreaterthandogstreatedwithplacebo.Alldogsinthecapromorelingroupgainweightby0.52kg,morethanthatofplacebogroup.Capromorelinshowsenhancedintestinalabsorptioninrodentmodelsandexhibitssuperiorpharmacokineticproperties,includinghighbioavailabilitiesintwoanimalspecies[F(rat)=65%,F(dog)=44%].CapromorelinstimulatesGHreleaseinanesthesizedratmodel,withED50of0.05mg/kgiv.
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