Drug concentration in STZ-induced diabetic peripheral neuropathic mechanical allodynia in overnight fasted Sprague-Dawley rat spinal cord at 1 mg/kg, po measured at 5.75 hrs post dose
Inhibition of bacterially expressed GST-Xa-tagged human AAK1 using 5-FAM-labelled Aha-KEEQSQITSQVTGQIGWR-NH2 peptide as substrate incubated for 3 hrs in presence of ATP by electrophoretic analysis
Displacement of 3H-LP-927443 from AAK1 in C57BL6 mouse brain homogenate assessed as inhibition constant incubated for 1 hr by liquid scintillation counter analysis
Inhibition of full length human AAK1 expressed in HEK293F cells assessed as suppression of AP2 phosphorylation measured after 3 hrs by Western blot analysis based cellular assay
Metabolic stability in human liver microsomes assessed as parent compound remaining at 0.5 uM incubated for 10 mins in presence of NADPH by LC-MS/MS analysis
Metabolic stability in rat liver microsomes assessed as parent compound remaining at 0.5 uM incubated for 10 mins in presence of NADPH by LC-MS/MS analysis
Metabolic stability in mouse liver microsomes assessed as parent compound remaining at 0.5 uM incubated for 10 mins in presence of NADPH by LC-MS/MS analysis
Ratio of drug concentration in spinal cord to plasma in CCI induced thermal hyperalgesia in Sprague-Dawley rat at 1 mg/kg, po measured at 5.5 hrs post dose
Plasma concentration in STZ-induced diabetic peripheral neuropathic mechanical allodynia in overnight fasted Sprague-Dawley rat at 1 mg/kg, po measured at 5.75 hrs post dose
Ratio of drug concentration in spinal cord to plasma in STZ-induced diabetic peripheral neuropathic mechanical allodynia in overnight fasted Sprague-Dawley rat at 1 mg/kg, po measured at 5.75 hrs post dose