HC-070 is a selective antagonist of TRPC4/TRPC5 channels, inhibiting hTRPC5 with an IC50 of 9.3 nM and hTRPC4 with an IC50 of 46 nM. It exhibits over 400-fold selectivity for human TRPC4/5 channels over other examined channels and weakly inhibits TRPC3 (IC50, 1 μM). It blocks various TRPC-mediated currents, including lanthanum-activated hTRPC5 and M2R-activated human TRPC1/TRPC4. In animal models, HC-070 has been shown to reduce CCK-4 evoked neuronal activity in the amygdala, decrease anxiety, and alleviate fear memory and marble burying behavior without affecting locomotor activity.
- Selective TRPC4/TRPC5 antagonist
- High selectivity for human TRPC4/5 channels
- Modulates TRPC-mediated currents
- Reduces neuronal activity
- Decreases anxiety and fear memory
- Reduces marble burying behavior