Probe | mol. wt.a | Apparent Permeability (Papp B→A)b | Postulated Binding Sitec | Comment | Reference |
---|---|---|---|---|---|
nm/s | |||||
Calcein-AM | 995 | N.D. | R,P | High throughput screening probe | Tiberghien and Loor, 1996; Polli et al., 2001; Schwab et al., 2003 |
Colchicine | 399 | 53 | H | Single binding site in Pgp | Shapiro and Ling, 1997; Martin et al., 2000 |
Digoxin | 781 | 16 | R | Clinically important probe | Englund et al., 2004; Keogh and Kunta, 2006 |
Prazosin | 382 | 283 | P | Historical probe for Pgp binding studies | Shapiro et al., 1999; Isenberg et al., 2001 |
Vinblastine | 811 | 97 | R | Historical probe for multidrug resistance | Doppenschmitt et al., 1999 |
GF120918 | 564 | N.D. | M | Clinically significant inhibitor and research tool | Polli et al., 2001; Tang et al., 2002 |
N.D., not determined; R, rhodamine 123/anthracycline site; P, progesterone/prazosin site; H, Hoechst 33342 site; M, central modulation site.
↵ a Molecular weight of the free form.
↵ b Apparent permeability in the presence of the Pgp inhibitor GF120918 (5 μM).
↵ c Shapiro and Ling, 1997; Martin et al., 2000; Lugo and Sharom, 2005.