Carbamazepine is an inhibitor of sodium channels. It preferentially inhibits inactivated voltage-gated sodium channel Nav1.7 and Nav1.3 (IC50s = 406 and 900 µM, respectively) over resting (closed) Nav1.7 and Nav1.3 channels in whole-cell patch-clamp assays using HEK293 cells (IC50s = 1,584 and 2,464 µM,...

Ticagrelor is a reversible antagonist of the platelet purinergic P2Y12 receptor (Ki = 14 nM, IC50 = 1.8 µM), which is the main receptor responsible for ADP-induced platelet aggregation. It functions by directly changing the conformation of the P2Y12 receptor to inhibit ADP binding. Formulations containing ticagrelor...

9-Phenanthrol is an inhibitor of transient receptor potential melastatin 4 (TRPM4, IC50s = 19.1, 17.1, and 22.8 µM at +40, -40, and -80 mV, respectively, in HEK293 cells expressing the human receptor). It is selective for TRPM4 over TRPM5 at 100 µM. 9-Phenanthrol (100 µM) reduces heart rate in spontaneously beating...

Lamotrigine is an anticonvulsant. It inhibits voltage-gated sodium channels (Nav) in HEK293 cells expressing recombinant human Nav1.2, Nav1.5, or Nav1.8 (IC50s = 10, 62, and 96 µM, respectively), as well as high voltage-activated calcium currents in isolated rat cortical neurons (IC50 = 12.3 µM), an effect that can...