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MC4R activation in the hypothalamus PT-141 crosses the blood-brain barrier and activates MC4R in the hypothalamus , especially in two areas: Medial preoptic area (MPA) , the main center for integration of sexual behavior Paraventricular nucleus (PVN) , the coordinator of neuroendocrine and autonomic responses Activation of MC4R in these areas via Gαs → cAMP → PKA leads to: Increased dopaminergic signaling in dopaminergic pathways (especially the mesolimbic pathway with the reward system) Activation of oxytocinergic neurons Inhibition of prolactin (which is a libido suppressor) Modulation of serotonin in pathways negatively affecting sexual function Clinical manifestation The result of these central changes: Increased sexual desire Better subjective arousal In men: erections via centrally activated parasympathetic pathways In women: vaginal lubrication and clitoral arousal via autonomic pathways Difference from PDE5 inhibitors (Viagra) This is the key mechanistic difference : PT-141 thus acts at the level of desire and arousal in the brain , while Viagra acts at the level of vascular response in the genitals
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