Bidirectional transport of 5-HT1B/1D agonists across LLC-PK1, LLC-MDR1, and LLC-Mdr1a cell monolayers
Analytea | LLC-PK1 | MDR1 | Mdr1a | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
BA/AB Ratio
|
% Transport at t = 4
hb |
BA/AB Ratio
|
% Transport at t = 4
hb |
BA/AB Ratio
|
% Transport at t = 4
hb | ||||||||||
|
A to B
|
B to A
|
A to B
|
B to A
|
A to B
|
B to A
| ||||||||||
| Eletriptan | 1.5 | 13 | 23 | 11 | 2.5 | 32 | 9.1 | 3.3 | 38 | ||||||
| Naratriptan | 1.3 | 3.1 | 3.8 | 3.2 | 1.2 | 4.1 | 2.1 | 3.4 | 6.3 | ||||||
| Rizatriptan | 1.1 | 4.9 | 4.9 | 3.2 | 2.3 | 8.2 | 2.1 | 2.9 | 8.6 | ||||||
| Sumatriptan | 1.5 | 1.6 | 3.0 | 2.7 | 1.2 | 4.2 | 1.1 | 2.9 | 3.5 | ||||||
| Zolmitriptan | 1.0 | 2.2 | 2.5 | 2.2 | 1.4 | 2.9 | 1.2 | 3.2 | 3.7 | ||||||
| Dexamethasone | 1.3 | 14 | 18 | 4.3 | 6.1 | 26 | 4.5 | 6.1 | 25 | ||||||
| Ritonavir | 1.3 | 18 | 24 | 27 | 1.2 | 29 | 11 | 2.5 | 25 | ||||||
|
Verapamil
|
1.4
|
18
|
24
|
4.9
|
5.4
|
33
|
6.3
|
5.8
|
38
| ||||||
↵ a Substrate concentrations were 10 μM for ETT, NARA, RIZA, SUMA, and ZOLM, 0.5 μM for verapamil, and 5 μM for ritonavir and dexamethasone.
↵ b Analyses were performed in triplicate and mean data are expressed to two significant figures (percentage CVs were <10% for ETT and <30% for NARA, RIZA, SUMA, and ZOLM).