Avanafil CAS# 330784-47-9 阿伐那非

Avanafil is a highly selective phosphodiesterase-5 (PDE5) inhibitor with potent in vitro activity, exhibiting an IC₅₀ of ~5 nM against human PDE5, while showing >100-fold selectivity over PDE6 and >10,000-fold over most other PDE isoforms, minimizing off-target effects. In isolated corpus cavernosum smooth muscle, avanafil enhances nitric-oxide–mediated cGMP accumulation and induces concentration-dependent relaxation at nanomolar to low-micromolar ranges. In vivo, avanafil significantly improves erectile responses in animal models of erectile dysfunction, including diabetic and aged rats, increasing intracavernosal pressure/mean arterial pressure ratios after oral dosing (typically 0.3–10 mg/kg). These effects correlate with enhanced penile blood flow and smooth muscle relaxation without significant cardiovascular or retinal adverse effects, supporting its rapid-onset, peripherally selective PDE5 inhibition profile.