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PF-00446687 is a potent and selective small molecule agonist of the melanocortin 4 receptor (MC4R), developed by Pfizer for the treatment of erectile dysfunction. It is brain penetrant and acts as a non-peptide agonist with high selectivity for MC4R. In clinical studies up to phase II for erectile dysfunction in men, a single oral dose of 200 mg showed similar effectiveness to 100 mg sildenafil; lower doses were ineffective. The drug demonstrated that selective targeting of MC4R can produce aphrodisiac effects comparable to older peptide-based melanocortin receptor agonists but with fewer side effects due to its selectivity[1][2][3][7].
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