Table 4.
In vivo CO exposure versus physicochemical properties of prodrugs.
| Compound | t1/2(h) | COHb AUC (%·h) | Oral absorption of intact CO prodrugs | Ranking of lipophilicity (1 being strongest) |
|---|---|---|---|---|
| CO-103 | 0.4 | 4.1 ± 0.3 | Yes | 2 |
| CO-125 | 0.8 | 6.1 ± 1.4 | No | 3 |
| CO-116 | 1.6 | 5.6 ± 1.1 | No | 4 |
| CO-104 | 4.2 | 2.3 ± 0.4 | Yes | 1 |
| CO-115 | 6.4 | 2.2 ± 0.5 | No | 5 |
t1/2: release half-life of CO prodrug in SIF (50% DMSO); COHb AUC: area under the curve for blood COHb level subtracting the pre-administration baseline from time zero to the last sampling time point. Results are presented as the mean ± SD (n ≥ 3).