N-Nornuciferine

N-Nornuciferine is an aporphine alkaloid derived from lotus leaf that strongly inhibits CYP2D6 with an IC50 of 3.76 ?M and Ki of 2.34 ?M, and pharmacokinetic studies show rapid absorption into blood with mean Cmax values of 1.71 ?g/mL at 0.9 h and 0.57 ?g/mL at 1.65 h after administration. Following intravenous dosing at 10 mg/kg, N-Nornuciferine exhibits a wide volume of distribution of 9.48–15.17 L/kg and slow elimination half-lives of 2.09–3.84 h. the oral bioavailability of N-Nornuciferine is estimated at 58.13–79.91%. At 20 mg/kg i.v. dosing, N-Nornuciferine also rapidly crosses the blood–brain barrier, achieving unbound Cmax values of 0.32 ?g/mL and 0.16 ?g/mL at approximately 0.89–1.22 h.