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ASP2205 is a potent and selective small molecule agonist of the serotonin 5-HT2C receptor. It was developed to enhance pudendal nerve-mediated urethral closure reflexes via activation of the 5-HT2C receptor, with the aim of preventing involuntary urine loss. In preclinical studies, ASP2205 demonstrated high selectivity and potency for human and rat 5-HT2C receptors (EC50 values of 0.85 nM and 2.5 nM, respectively). However, in clinical trials involving healthy volunteers, ASP2205 did not increase urethral pressure or show efficacy for stress urinary incontinence; it was also associated with central nervous system-related side effects such as dizziness and nausea[1][10][7]. The drug is not approved for any indication.
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