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The sole member of a class of synthetic products that mimic naturally occurring PGE1. It activates adenylate cyclase, which synthesizes cAMP from ATP. cAMP acts as a second messenger activating protein kinase A, which results in an efflux of intracellular calcium and subsequent smooth-muscle relaxation and the development of an erection.
Sexual stimulation is required to initiate activation of NOS of nitric oxide, which is released from endothelial cells and cavernous nerves to stimulate guanylyl cyclase, resulting in increased levels of cGMP. Subsequent phosphorylation of cellular membrane proteins via protein kinase G results in an efflux of calcium, which leads to vascular smooth-muscle relaxation. By blocking cGMP breakdown, these drugs produce a more profound sustained relaxation of the vascular smooth muscle, leading to an erection.
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