MAO-B-IN-20

MAO-B-IN-20 (Compound C14; 5 mg/kg; i.v.) is rapidly absorbed and crossed the blood-brain barrier within 15 min, reaching the C_max in 60 min in both plasma and brain. MAO-B-IN-20 exhibits an adequate brain to plasma ratio of 16.20 and high concentration in brain (8753 ng/g) at 60 min^[1].
MAO-B-IN-20 (0.08-1.28 mg/kg; i.p.; once) prominently inhibits the MAO-B activity in a dose-dependent manner in the mouse brain^[1].
MAO-B-IN-20 (0.3-3 mg/kg; i.p.; once) exhibits a potential efficacy for dopamine deficits in the MPTP (HY-15608)-induced mouse model and significantly increased dopamine concentration in the striatum^[1].
Pharmacokinetic profile of MAO-B-IN-20 (Compound C14) in SD rats^a[1]

Compound	Route	Dose (mg/kg)	Cmax (ng/mL)	AUCt (ng•h/mL)	T1/2 (h)	Vss (L/kg)	CL (mL/min/kg)	F (%)
MAO-B-IN-20 (Compound C14)	iv	1	273	305	0.74	3.33	54.2	/
	ig	5	436	2280	4.22	/	/	149.5

^aFasted male SD rats. Dosing volumes: 5 mL/kg for ig and 1 mL/kg for iv. C_max: Maximum Concentration, AUC_t: Area under the plasma concentration-time curve from time 0 to last time of quantifiable concentration; T_1/2: Elimination half time, V_ss: Steady-state distribution volume, CL: plasma clearance, F: bioavailability.
Pharmacokinetic profile of MAO-B-IN-20 (Compound C14) in ICR mice^a[1]

Compound	Route	Dose (mg/kg)	Cmax (ng/mL)	AUCt (ng•h/mL)	T1/2 (h)	Vss (L/kg)	CL (mL/min/kg)	F (%)
MAO-B-IN-20 (Compound C14)	iv	2	900	2680	3.37	2.72	11	/
	ig	5	913	7950	3.80	/	/	104.8

^aFasted male ICR mice. Dosing volumes: 5 mL/kg for ig and 2 mL/kg for iv. C_max: Maximum Concentration, AUC_t: Area under the plasma concentration-time curve from time 0 to last time of quantifiable concentration; T_1/2: Elimination half time, V_ss: Steady-state distribution volume, CL: plasma clearance, F: bioavailability.