Optical control of the cardiac rhythm with photoswitchable NaV1.5 channel blockers - PubMed
a day ago
- #optopharmacology
- #NaV1.5
- #cardiac rhythm
- NaV1.5 channel is crucial for cardiac excitability and is a target for treating arrhythmias.
- Quinidine is an effective NaV1.5 blocker but lacks specificity.
- A photoswitchable quinidine derivative, azo-Q2a, was developed for optical control of NaV1.5.
- azo-Q2a shows high selectivity for NaV1.5 and minimal off-target effects.
- The cryo-EM structure of NaV1.5 with azo-Q2a reveals the binding site for optical control.
- azo-Q2a can modulate heart rate in zebrafish larvae, indicating potential therapeutic applications.