etripamil CAS# 1593673-23-4 艾曲帕米

Etripamil is a potent, short‑acting L‑type calcium channel blocker that inhibits calcium influx and prolongs atrioventricular nodal refractory periods in vitro via Cav1.2/Cav1.3 channel blockade (electrophysiological inhibition of AV nodal conduction seen in calcium channel assays). In conscious cynomolgus monkeys, intravenous etripamil produces dose‑dependent increases in PR interval (e.g., ~27% prolongation at 0.3 mg/kg), decreases systolic blood pressure, increases heart rate, and shows plasma Cₘₐₓ up to ~176 ng/mL with half‑lives ~12–21 min, consistent with rapid onset and short duration of action. Repeated intranasal doses (1.9–5.7 mg/kg weekly) in macaques cause transient local effects without systemic toxicity. These preclinical functional data align with its mechanism for stopping supraventricular tachyarrhythmias.