Extended Data Fig. 5: Pharmacokinetic properties of Muzepan1 and Muzepan2.
From: GTP release-selective agonists prolong opioid analgesic efficacy
a. Brain and plasma levels measured in male C57BL6/J mice at the indicated time points; means with SD are shown (muzepan1: 3 mg/kg, n = 6 plasma, 3 brain; 24 mg/kg n = 3 plasma, 4 brain; muzepan2: 3 mg/kg: n = 3 plasma, 3 brain; 24 mg/kg, n = 4 plasma, 4 brain). The conversion of tissue levels to molarity assumes 1 gram = 1 mL. b. Single point (10 µM) inhibition of cytochrome P450 enzymes presented as % inhibition and comparison to known standard inhibitors performed in duplicate.
