Table 5.

Preliminary Pharmacokinetic Screen of 2,6-Dimethyl-4-fluoro B-SERDs Compared to 2^a

	plasma concentration (nM)		brain concentration (nM)
compound	0.5 h	2 h	0.5 h	2h
2	31.2 ± 16.5	301 ± 268	0.7 ± 0.8b	47.4 ± 61.1
30f	786 ± 179	659 ± 329	750 ± 673	588 ± 274
30m	211 ± 45	163 ± 141	121 ± 61	276 ± 93
37d	2490 ± 797	2150 ± 201	1630 ± 1110	1250 ± 406

^aPlasma and brain concentration of 30f, 30m and 37d (100 mg/kg p.o.), and 2 (5 mg s.c.) showing mean and s.d. (N = 3).

^bBelow LOQb_rain = 5nM.