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Toxicity in FVB mouse assessed as tolerance
Assay data:1 Tested
SummaryPubMed Citation
Drug concentration in plasma of orally dosed formalin-induced FVB mouse model of pain measured after 3 hrs by UPLC-ESI MC/MC analysis
Brain to plasma ratio in FVB mouse model of aconitine-induced pain expressing human Nav1.7 I848T mutant administered orally 120 mins prior to aconitine administered and measured after 70 mins by UPLC-ESI MS/MS analysis
Drug concentration in brain of FVB mouse model of aconitine-induced pain expressing human Nav1.7 I848T mutant at 10 mg/kg, po administered 120 mins prior to aconitine administered and measured after 70 mins by UPLC-ESI MS/MS analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed Citation
Drug concentration in brain of FVB mouse model of aconitine-induced pain expressing human Nav1.7 I848T mutant at 3 mg/kg, po administered 120 mins prior to aconitine administered and measured after 70 mins by UPLC-ESI MS/MS analysis
Drug concentration in plasma of FVB mouse model of aconitine-induced pain expressing human Nav1.7 I848T mutant at 10 mg/kg, po administered 120 mins prior to aconitine administered and measured after 70 mins by UPLC-ESI MS/MS analysis
Drug concentration in plasma of FVB mouse model of aconitine-induced pain expressing human Nav1.7 I848T mutant at 3 mg/kg, po administered 120 mins prior to aconitine administered and measured after 70 mins by UPLC-ESI MS/MS analysis
Unbound plasma concentration in FVB mouse model of aconitine-induced pain expressing human Nav1.7 I848T mutant at 0.3 mg/kg, po administered 120 mins prior to aconitine administration and measured after 70 mins by UPLC-ESI MS/MS analysis
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Antinociceptive activity against aconitine-induced pain in FVB mouse model expressing human Nav 1.7 I848T mutant assessed as reduction in nociceptive behavior at 10 mg/kg, po administered 120 mins prior to aconitine administration and measured after 70 mins relative to control
Antinociceptive activity against aconitine-induced pain in FVB mouse model expressing human Nav 1.7 I848T mutant assessed as reduction in nociceptive behavior at 3 mg/kg, po administered 120 mins prior to aconitine administration and measured after 70 mins relative to control
Antinociceptive activity against aconitine-induced pain in FVB mouse model expressing human Nav 1.7 I848T mutant assessed as reduction in nociceptive behavior at 1 mg/kg, po administered 120 mins prior to aconitine administration and measured after 70 mins relative to control
Antinociceptive activity against aconitine-induced pain in FVB mouse model expressing human Nav 1.7 I848T mutant assessed as reduction in nociceptive behavior at 0.3 mg/kg, po administered 120 mins prior to aconitine administration and measured after 70 mins relative to control
Antinociceptive activity against aconitine-induced pain in FVB mouse model expressing human Nav 1.7 I848T mutant assessed as reduction in nociceptive behavior at 0.1 mg/kg, po administered 120 mins prior to aconitine administration and measured after 70 mins relative to control
Analgesic activity against formalin-induced pain in FVB mouse model assessed as reduction in formalin-induced pain at 10 mg/kg, po administered for 120 mins prior to formalin challenge and measured after 11 to 40 mins
Oral bioavailability in Beagle dog at 1 mg/kg
AUC in Beagle dog at 1 mg/kg, po
Cmax in Beagle dog at 1 mg/kg, po
Half-life in Beagle dog at 1 mg/kg, po
Volume of distribution at steady state in Beagle dog at 0.5 mg/kg, iv
Clearance in Beagle dog at 0.5 mg/kg, iv
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