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Positive inotropic activity in ferret papillary muscle assessed as contractile force measured as CFC20
Assay data:3 Active, 2 Activity ≤ 1 µM, 4 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Prodrug conversion in ferret lung assessed as triphosphate metabolite formation at 10 mg/kg, iv measured after 24 hrs
Assay data:1 Tested
SummaryPubMed Citation
Prodrug conversion in ferret assessed as AUC (0 to last) of parent nucleoside compound at 10 mg/kg, iv
AUC (0 to infinity) in ferret at 10 mg/kg, iv
Volume of distribution at steady state in ferret at 10 mg/kg, iv
Half life in ferret at 10 mg/kg, iv
Clearance in ferret at 10 mg/kg, iv
Toxicity in ferret assessed as induction of emesis at 10 umol/kg, IT measured for 4 hrs
Assay data:2 Tested
Toxicity in ferret assessed as induction of emesis at 1 umol/kg, IT measured for 4 hrs
Toxicity in ferret assessed as nausea-like score at 1 umol/kg, IT observed for 4 hrs (Rvb= 12.83+/-5.10)
Toxicity in ferret assessed as nausea-like score at 10 umol/kg, IT observed for 4 hrs (Rvb= 12.83+/-5.10)
Cmax in ferret at 0.25 mg/kg, iv
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Oral bioavailability in ferret
Toxicity in ferret assessed as induction of emesis at 0.25 mg/kg, iv
Induction of emesis in ferret up to 30 mg/kg, po
In vivo antagonist activity at mu-opioid receptor in sc dosed ferret assessed as inhibition of morphine-induced emesis/vomiting
In vivo antagonist activity at mu-opioid receptor in po dosed ferret assessed as inhibition of morphine-induced emesis/vomiting
Assay data:4 Tested
Toxicity in it dosed ferret assessed as emesis administered as dry powder co-mixtured with lactose after 1 hr post dose
Toxicity in ferret assessed as emesis at 30 ug/kg, it administered as dry powder co-mixtured with lactose after 1 hr post dose
Toxicity in ferret assessed as emesis at 3.5 umol/kg administered 30 mins prior to agonist treatment measured for 90 mins in presence of 5-[(2R)-Azetidin-2-yl methoxy]-2-chloropyridine
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