Erections are caused by increased blood flow from the relaxation of penile arteries and corpus cavernosal smooth muscle. Cyclic GMP (cGMP) causes smooth muscle relaxation and increased blood flow into the corpus cavernosum. During sexual stimulation, tadalafil will inhibit phosphodiesterase type 5 PDE5, which increases the amount of cGMP in smooth muscles cells thus enhancing erectile function.
Preclinical studies showed that tadalafil is over 10,000-fold more potent for PDE5 than for PDE1, PDE2, PDE4, and PDE7 enzymes, which are found in the heart, brain, blood vessels, liver, leukocytes, skeletal muscle, and other organs.
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