Table 4.

In vivo PK parameters and microsome stability for selected AMT analogs following a single 10 mg/kg oral dose in mice.

Cmpd	Cmax (μM) Brain	AUC (μM *h)		T1/2[a] (min)	Brain AUC/EC50 [b]
		Brain	Plasma
1	2.45 ± 0.74	9.78 ± 2.07	6.99 ± 0.73	> 60	7.6
12	0.50 ± 0.05	1.68 ± 0.10	ND[c]	>60	19
15	2.46 ± 0.85	10.90 ± 1.75	15.60 ± 0.06	>60	160
26	0.33 ± 0.16	1.04 ± 0.13	ND[c]	ND[c]	6.8
32	1.17 ± 0.19	5.22 ± 0.10	1.57 ± 0.15	6.8	6.9
27	0.97 ± 0.22	3.27 ± 0.44	6.75 ± 0.45	>60	24
16	0.90 ± 0.24	3.85 ± 0.52	11.50 ± 0.71	>60	19
34	4.34 ± 0.53	18.60 ± 3.75	12.70 ± 1.11	>60	75
45	0.25 ± 0.11	1.29 ± 0.02	0.76 ± 0.01	4.4	1.9
46	0.15 ± 0.01	0.32 ± 0.00	0.26 ± 0.01	55	2.7
47	0.06 ± 0.03	0.19 ± 0.08	0.38 ± 0.19	2.5	2.7

^[a]stability to mouse liver microsomes.

^[b]Ratio of brain AUC (μM *h) to EC₅₀ (μM).

^[c]not determined.