Table 2 Pharmacokinetic (PK) parameters of JH-ENT-01 and dilazep
From: Design of an equilibrative nucleoside transporter subtype 1 inhibitor for pain relief
| Â | JH-ENT-01 | Dilazep | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|
PK PARAMETER | Plasma | Brain | Spinal Cord | TG | DRG | Plasma | Brain | Spinal Cord | TG | DRG |
Tmax (time of Cmax)Â [h] | 0.50 | 1.50 | 0.50 | 1.50 | 0.17 | 0.50 | 0.17 | 1.50 | 1.50 | 0.17 |
Cmax (maximum observed concentration)Â [ng/mL] | 164 | 309 | 97 | 159 | 641 | 409 | 166 | 313 | 525 | 1531 |
Tlast (time of last measurement)Â [h] | 24 | 24 | 12 | 24 | 24 | 8 | 8 | 8 | 8 | 24 |
Clast (conc. at Tlast) [ng/mL] | 0.26 | 3.27 | 6.99 | 3.83 | 4.25 | 0.51 | 0.67 | 0.93 | 2.80 | 1.64 |
AUClast (area 0-Tlast) [h ng/ mL] | 760 | 1630 | 588 | 1042 | 2647 | 588 | 482 | 865 | 1340 | 1620 |
AUCinf (area 0-infinity) [h ng/mL] | 761 | 1646 | 609 | 1084 | 2677 | 589 | 483 | 866 | 1345 | 1641 |
t1/2 (terminal half-life) [h] | 2.48 | 3.38 | 2.13 | 7.56 | 4.91 | 0.83 | 0.84 | 0.78 | 1.23 | 9.05 |
Vz/F (volume of distr. based on terminal phase) [L/kg] | 141 | 89 | 152 | 302 | 79 | 61 | 75 | 39 | 39 | 239 |
Cl/F (clearance as Dose/AUCinf) [L/h/ kg] | 39 | 18 | 49 | 28 | 11 | 51 | 62 | 35 | 22 | 18 |
MRTinf (mean residence time, 0-infinity) [h] | 3.75 | 4.62 | 4.01 | 4.87 | 4.65 | 1.29 | 1.72 | 1.50 | 1.50 | 1.64 |
