In vivo evidence of the presence of ABC transporters in the heart by the use of knockout mice
| ABC Transporter Studied | Mice Type | Reference |
|---|---|---|
| mdr1a/1b (P-gp or ABCB1) | ||
| Vinblastine levels were about 3-fold higher in hearts of mdr1a–/– mice, which had a longer elimination vs. wild-type mice | mdr1a–/– and wild-type | Schinkel et al. (1994) |
| In mdr1a–/– mice, heart accumulated increased amounts of vinblastine vs. wild-type mice | mdr1a–/– and wild-type | van Asperen et al. (1996) |
| Tissue levels of radioactivity in some tissues, including the heart of mdr1a–/– mice, are 2-fold higher following administration of [3H]loperamide vs. wild-type mice | mdr1a–/– and wild-type | Schinkel et al. (1996) |
| A 1.7-fold increase in the accumulation of vinblastine was observed in the heart of mdr1a–/– mice vs. wild-type mice | mdr1a–/– and wild-type | van Asperen et al. (1999) |
| Tissues such as the heart displayed at least 2-fold higher tissue levels in mdr1a / 1b–/– following administration of enaminone anticonvulsants vs. wild-type mice | mdr1a / 1b–/– and wild-type | Cox et al. (2002) |
| mrp1 (ABCC1) | ||
| There was increased toxicity in the TKO mice that accumulated etoposide in some tissues such as the heart vs. DKO mice | DKO, TKO, and wild-type | Wijnholds et al. (2000) |
| A higher tissue/plasma ratio was observed in some tissues such as the heart in mrp1–/– following administration of grepafloxacin vs. wild-type mice | mdr1a / 1b–/–, mdr1a–/–, mrp1–/–, and wild-type | Sasabe et al. (2004) |
| mdr1a/1b (P-gp or ABCB1) and mrp1 (ABCC1) | ||
| Vincristine tissue/plasma ratio comparisons showed higher values in the heart of both weanling and adult combined mdr1a / 1b–/–, mrp1–/– mice than in wild-type mice | TKO and wild-type | Muramatsu et al. (2004) |
DKO, mdr1a and mdr1b double-knockout mice (or mdr1a / 1b–/–); TKO, mrp1, mdr1a and mdr1b triple-knockout mice (or mrp1–/–/mdr1a / 1b–/–)