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Cialis, siklik guanozin monofosfata (cGMP) özgü fosfodiesteraz tip 5'in (PDE5) etkili, geri dönüşümlü ve seçici bir inhibitörüdür. Cinsel uyarılma lokal nitrik oksit salınımına neden olduğunda, Cialis'in PDE5'i inhibe etmesi, penisin korpus kavernozasında cGMP seviyelerinde artışa yol açar.
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