Tariquidar

Tariquidar is an anthranilic acid derivative that binds to P-glycoprotein (K_d = 5.1 nM) and inhibits transport activity.¹ It inhibits transport of vinblastine (Item No. 11762) and paclitaxel (Item No. 10461) in multidrug resistant CH^rB30 cells, increasing the steady state accumulation to non-P-glycoprotein-expressing multidrug sensitive cell levels (EC₅₀ = 487 nM). Tariquidar also enhances the distribution of its substrates, increasing the amount of substrate entering the CNS.² When administered at doses of 2 and 6.25 mg/kg in mice in combination with the peripherally-restricted opioid loperamide, the latency to paw withdrawal in a hot plate assay increases, indicating that loperamide is transported into the CNS.

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1. Martin, C., Berridge, G., Mistry, P., et al. The molecular interaction of the high affinity reversal agent XR9576 with P-glycoprotein. Br. J. Pharmacol. 128(2), 403-411 (1999).

2. Choo, E.F., Kurnik, D., Muszkat, M., et al. Differential in vivo sensitivity to inhibition of P-glycoprotein located in lymphocytes, testes, and the blood-brain barrier. J. Pharmacol. Exp. Ther. 317(3), 1012-1018 (2006).