. Author manuscript; available in PMC: 2020 Mar 20.

Published in final edited form as: ACS Chem Neurosci. 2018 Dec 14;10(3):1679–1695. doi: 10.1021/acschemneuro.8b00600

Table 2.

Brain/Plasma Pilot PK Studies and Initial ADMET Evaluation of SW-100^a

brain/plasma PK studies
route	dose (mg/kg)	time (h)	brain concn (ng/mL)	plasma concn (ng/mL)	brain/ plasma ratio
IP	20	1	141.8 ± 52.3	58.2 ± 24.9	2.44
IP	20	4	11.5 ± 0.30	2.52 ± 0.13	4.54
ADMET parameters
liver microsomal stability (t_1/2 min)			human		23
			mouse		23
hepatocyte stability (t_1/2, min)			human		30
			mouse		10
hERG test (IC₅₀, μM)			HEK293 cells		12.23
CYP inhibition (% @10 μM)			1A2		20.53
			2C9		18.84
			2C19		83.21
			2D6		2.51
			3A4		−0.63
Ames test			TA98, TA100, TA1535, TA1537, WP2 uvrA		negative

SW-100 was administered to C57BL/6 male mice by IP administration at the dose of 20 mg/kg. Blood and brain samples were collected at 1 and 4 h time points. Brain tissues were homogenized at a 1:4 ratio of tissue weight (g) to volume of PBS (mL). The data found (ng/mL) was multiplied by 5 to obtain the concentration (ng/mL) in brain tissues. PK studies and ADMET profiles were conducted by Pharmaron, Inc., Irvine, CA.