Avanafil is a potent and highly selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 of 5.2 nM for erectile dysfunction, exhibiting lower selectivity against PDE1, PDE6, and PDE11.
Avanafil (TA-1790) exhibits strong and specific inhibitory effects on phosphodiesterase-5 (PDE-5), with IC50 values being 5.2 nM for PDE-5 and progressively higher for PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2, and PDE-1. It enhances the NO/cGMP/PKG signaling pathway, leading to a reduction in bone mineral density (BMD) loss, bone weakening, and oxidative stress. By preventing the breakdown of cyclic guanosine monophosphate (cGMP), Avanafil elevates cGMP levels, making it a candidate for studies on erectile dysfunction and osteoporosis[1][2][3].
体内研究
Administered orally at 10 mg/kg daily for 30 days to male rats, Avanafil (TA-1790) promotes angiogenesis in bone tissue through the NO/cGMP/PKG pathway and notably reduces the dexamethasone-induced decrease in BMD, bone deterioration, and oxidative stress[1].
体外研究
In corpus cavernosum strips from diabetic subjects, Avanafil (TA-1790) at concentrations ranging from 0.01 to 1000 µM increases the relaxation response induced by electrical field stimulation (1-20 Hz) by 45%[2].
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