Table 5. Assessment of in vivo exposure parameters of 1e and two novel M4 mAChR PAMs.
Cpd | 20 or 30 min post-dose | 90 min post-dose | |||
---|---|---|---|---|---|
Cplasma | Cbrain | Cplasma | Cbrain | k p | |
nM | nM | nM | nM | ||
1e | 2438 ± 858 | 481 ± 169 | 14 ± 6 | 9 ± 5 | 0.1−0.3 |
6k | 915 ± 402 | 2144 ± 1097 | 159 ± 64 | 255 ± 107 | 1.6−2.5 |
6l | 2427 ± 111 | 982 ± 74 | 657 ± 35 | 373 ± 17 | 0.3−0.6 |
Data is presented as average ± SEM (n = 2–3/drug/time point), or range for Kp value.